JAK
信号通路图
研究领域
抑制剂选择性比较
JAK产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1378 |
Ruxolitinib (INCB018424)Ruxolitinib (INCB018424)是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1， JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。 |
STAT3 phosphorylation as determined by phospho flow, mixed lymphocyte reactions containing BALB/c spleen-derived CD4+ T cells co-cultured with or without C57BL/6 BM-derived DC preactivated with 20 ng/mL LPS.
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| S5001 |
Tofacitinib (CP-690550) CitrateTofacitinib citrate (CP-690550, Tasocitinib)是一种新型JAK抑制剂，对JAK3，JAK2，JAK1的IC50分别为1 nM, 20 nM 和112 nM。Tofacitinib citrate 还具有抗感染的活性。 |
CP-690550 reduced the severity of ischemic damage. (A) CP-690550 (10 μM) suppressed IL-17 production by cdT cells and activated memory T cells. cdT cells and CD4+ CD44+ memory T cells isolated from C5BL6J mice through flow cytometry were stimulated for 24 h with plate-bound monoclonal antibodies to CD3 (2 ng/ml) and CD28 (1 ng/ml) in the presence or absence of IL-23 (25 ng/ml). IL-17A production and IL-17A expression level were measured by quantitative RT-PCR (a) and ELISA (b). (B) CBF reduction after brain ischemia. (C) Time-dependent changes in neurological score. *p < 0.05. (D) Infarct volume as visualized through TTC staining on day 3 in CP-690550 (CP)- and vehicle-treated mice.
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| S2162 |
AZD1480AZD1480是一种新型，ATP竞争性的JAK2抑制剂，无细胞试验中IC50为0.26 nM，选择性作用于JAK3和Tyk2，对JAK1的作用较弱。Phase 1。 |
HEL cells were treated for 3 hours with the indicated concentrations of AZD1480. AZD1480 inhibits Jak2-V617F mediated signal transduction at micromolar concentrations in intact cells.
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| S2736 |
Fedratinib (TG101348)Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3) 和 Ret (c-RET)，对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。 |
Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.
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| S1134 |
AT9283AT9283是一种有效的JAK2/3抑制剂，无细胞试验中IC50为1.2 nM/1.1 nM；对Aurora A/B，Abl1(T315I)也有效。Phase 2。 |
HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
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| E0933New |
AristolactamAristolactam (Aristolactam I) is the main active ingredient in the Aristolochia plant species, which have been associated with severe nephrotoxicity. |
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| S7002New |
ZotiraciclibZotiraciclib (SB1317; TG02)是一种新型小分子CDK/JAK2/FLT3抑制剂，对CDK1、2和9的IC50分别为9、5和3 nM，抑制FLT3的IC50为19 nM，抑制JAK2的IC50为19 nM。 |
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| S8152New |
Cucurbitacin ICucurbitacin-I (Elatericin B, JSI 124, NSC 521777)，一种从葫芦科植物中分离出来的天然细胞渗透性三萜，是一种新型的 JAK2/STAT3 选择性抑制剂。 |
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| S6789New |
JAK Inhibitor I (Pyridone 6)JAK Inhibitor I (Pyridone 6, CMP 6, Compound 6) 是一种泛 JAK 抑制剂，对JAK2, TYK2, JAK3 和 JAK1 的IC50分别为 1 nM, 1 nM, 5 nM 和 15 nM。 |
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| E0011New |
LinderalactoneLinderalactone 通过调节 A-549 细胞中 凋亡相关蛋白（Bax 和 Bcl-2） 的表达来抑制人肺癌的生长，IC50 为 15 µM。Linderalactone 诱导 G2/M 细胞周期停滞，还可以抑制 JAK/STAT 信号通路。Linderalactone 可以从 Radix linderae 中分离出来。 |
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| S1143 |
AG-490 (Tyrphostin B42)AG-490 (Tyrphostin B42, Zinc02557947) 是一种EGFR抑制剂，在无细胞试验中IC50为0.1 μM，作用于EGFR比作用于ErbB2选择性高135倍，对JAK2也有抑制作用，对Lck，Lyn，Btk，Syk和Src没有抑制活性。 |
Inhibition of JAK1/2 with AG490 or STAT3 with S3I-201 leads to reduced STAT3 activation and reduced WASF3 levels. In contrast, treatment with Dasatinib (SRC inhibitor) or Gefitinib (EGFR inhibitor) does not significantly affect activated STAT3 or WASF3 levels
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| S2219 |
Momelotinib (CYT387)Momelotinib (CYT387, LM-1149 , CYT11387) 是一种ATP竞争性JAK1/JAK2抑制剂，IC50为11 nM/18 nM，比作用于JAK3选择性约高10倍左右。Momelotinib (CYT387) 可诱导凋亡和自噬。Phase 3。 |
IL-6- supported INA-6 cells were treated with the JAK inhibitors ruxolitinib (Rux; 10 nM) or CYT387 (CYT; 50 nM) for 1 hour and assessed for inhibition of STAT3 phosphorylation by immunoblotting.
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| S2789 |
Tofacitinib (CP-690550)Tofacitinib (CP-690550,Tasocitinib)是一种新型JAK3抑制剂，在无细胞试验中IC50为1 nM，作用于JAK2和JAK1选择性低20到100倍。Tofacitinib 可在人类浆细胞样树突状细胞PDC中抑制抗凋亡的BCL-A1和BCL-XL并诱导PDC凋亡。 |
TRAP-positive multinucleated cell differentiation depends on JAK and is inhibited by tofacitinib in vitro. Effect of tofacitinib on the differentiation of TRAP-positive multi-nucleated cells in vitro (n =3 wells/experiment). Original magnification x 100.
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| S2796 |
WP1066WP1066 是一种新型JAK2和STAT3抑制剂，在HEL细胞中IC50分别为2.30 μM和2.43 μM；对JAK2，STAT3，STAT5和ERK1/2具有抑制活性，而对JAK1和JAK3没有作用。WP1066 可诱导凋亡。Phase 1。 |
Effects of selective STAT3 inhibitors on adherent glioma CSCs. Cells were treated with WP1066 (50 uM for 2 h) or vehicle, and colocalization of STAT3 and p65 was determined by immunostaining.
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| S2692 |
TG101209TG101209是一种选择性的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET (c-RET)作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。 |
EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (*,P < 0.05; **, P < 0.01; ***, P < 0.001; NS, nonsignificant).
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| S2179 |
Gandotinib (LY2784544)Gandotinib (LY2784544)是一种有效的JAK2抑制剂，IC50为3 nM，作用于JAK2V617F有效，比作用于JAK1和JAK3选择性高8和20倍。Phase 2。 |
HEL cells were treated for 3 hours with the indicated concentrations of LY2784544. LY2784544 inhibits Jak2-V617F mediated signal transduction at submicromolar concentrations in intact cells.
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| S2686 |
NVP-BSK805 2HClNVP-BSK805 2HCl是一种有效的，选择性的，ATP竞争性的JAK2抑制剂，IC50为0.5 nM，比作用于JAK1， JAK3和TYK2选择性高20倍以上。 |
Determination of the kynurenine production in HFF cells after IDO induction by IFN-γ (100 U/mL). The cells were incubated for 72 h under normoxia (20% O2) or hypoxia (1% O2) and treated with different amounts of the JAK2 inhibitor BSK805 (0-2 uM).
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| S2851 |
Baricitinib (INCB028050)Baricitinib (LY3009104, INCB028050)是一种选择性JAK1和JAK2抑制剂，无细胞试验中IC50分别为5.9 nM和5.7 nM，比作用于JAK3和Tyk2选择性高70和10倍左右，对c-Met和Chk2没有抑制作用。Baricitinib被发现可以减少或干扰病毒进入目标细胞，并用于COVID-19的治疗研究中。Phase 3 |
bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test. |
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| S2214 |
AZ 960AZ 960 是一种新型的，ATP竞争性的JAK2抑制剂，IC50和Ki分别低于3 nM和0.45 nM，作用于JAK2比作用于JAK3选择性高3倍。AZ 960 可诱导凋亡和生长阻滞。 |
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| S2806 |
CEP-33779CEP-33779是一种选择性JAK2抑制剂，IC50为1.8 nM，比作用于JAK1和TYK2选择性高40多倍和800多倍。 |
Potentiation of the antitumor effects of vincristine by CEP-33779 in a KBv200 cell xenograft model in nude mice. (A) The changes in tumor volume with time after tumor cell implantation. (B) The photograph of tumor size was taken on the 21st day after implantation. The various treatments were as follows: (a) Control (vehicle alone); (b) Vincristine (q2d x 6, ip, 0.2 mg/kg); (c) CEP-33779 (q2d x 6, p.o, 30 mg/kg) and (d) Vincristine (q2d x 6, ip, 0.2 mg/kg) plus CEP-33779 (q2d ?6, p.o, 30 mg/kg, given an hour before Vincristine administration).
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| S8057 |
Pacritinib (SB1518)Pacritinib (SB1518)是有效的选择性Janus Kinase 2 (JAK2)和Fms-Like Tyrosine Kinase-3 (FLT3)抑制剂，无细胞试验中IC50分别为23和22 nM。Phase 3。 |
Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting
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| S2867 |
WHI-P154WHI-P154是一种有效的JAK3抑制剂，IC50为1.8 μM，对JAK1和JAK2没有抑制活性，也抑制EGFR， Src， Abl， VEGFR和MAPK，抑制Stat3而非Stat5磷酸化。 |
Reversal effect of WHI-P154 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without WHI-P154. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line. |
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| S7198 |
BIOBIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052)是一种特异性的GSK-3抑制剂，无细胞试验中作用于GSK-3α/β的IC50为5 nM，比作用于CDK5选择性高16倍以上，也是一种泛JAK抑制剂，对 Tyk2 的IC50值为30 nM。BIO 可在人类黑色素瘤细胞中诱导凋亡。 |
Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.
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| S7036 |
XL019XL019是一种有效的，选择性的JAK2抑制剂，IC50为2.2 nM，比作用于JAK1， JAK3和TYK2.选择性高50倍。Phase 1。 |
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| S2902 |
S-Ruxolitinib (INCB018424)S-Ruxolitinib (INCB018424)是第一个应用到临床的，有效的，选择性JAK1/2抑制剂，IC50为3.3 nM/2.8 nM，作用于JAK1/2比作用于JAK3选择性高130倍以上。 Phase 3。 |
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| S8004 |
ZM 39923 HClZM 39923 HCl是一种JAK1/3抑制剂，pIC50为4.4/7.1，对JAK2没有作用活性，适度有效作用于EFGR；对转谷氨酰胺酶敏感。 |
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| S6899 |
Licochalcone DLicochalcone D (Lico D, LCD, LD) 是一种从中草药甘草 Glycyrrhiza inflata 中分离出的类黄酮，具有抗氧化、抗炎和抗癌的特性。Licochalcone D 可抑制LPS信号通路中NF-κB p65的磷酸化。Licochalcone D 可抑制 JAK2、EGFR 和 Met (c-Met) 活性，并诱导ROS依赖性的凋亡。Licochalcone D 还可诱导 caspases 的活化和 poly (ADP-ribose) polymerase (PARP) 的裂解。 |
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| S6521 |
WHI-P258WHI-P258是JAK3的抑制剂，Ki值为72 μM。 |
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| S0918 |
Ginkgolic acid C17:1Ginkgolic acid C17:1 (GAC 17:1) 通过废除上游的 JAK2 和 Src 来抑制 STAT3 的组成性激活。Ginkgolic acid C17:1 可以诱导 PTEN 和 SHP-1 的大量表达。Ginkgolic acid C17:1 诱导肿瘤细胞凋亡。 |
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| S3267 |
Kaempferol-3-O-rutinosideKaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside) 是从 Carthamus tinctorius 中提取的黄酮，可改变受伤神经元的形状和结构，减少凋亡细胞，下调 p-JAK2、p-STAT3、caspase-3 和 Bax 的表达，并降低Bax免疫反应性，并增加 Bcl-2 蛋白表达和免疫反应性。 |
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| S8538 |
Ritlecitinib (PF-06651600)Ritlecitinib (PF-06651600)是JAK3选择性的抑制剂，IC50为33.1 nM。对JAK1、JAK2和TYK2没有活性(IC50 > 10 000 nM)。 |
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| S5554 |
Lanatoside CLanatoside C 是具有抗病毒和抗肿瘤活性的强心苷。Lanatoside C 通过减弱 MAPK，Wnt，JAK-STAT和PI3K/AKT/mTOR信号通路，诱导G2/M细胞周期停滞并诱导自噬和细胞凋亡。 |
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| S5243 |
Ruxolitinib PhosphateRuxolitinib Phosphate (INCB018424, INC424)是Ruxolitinib的磷酸盐形式。Ruxolitinib 是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1，JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。 |
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| S6524 |
NSC 42834NSC42834 (JAK2 Inhibitor V, Z3)是野生型JAK2和JAK2(V617F)自身磷酸化的抑制剂，IC50的范围为10-30 μM。 |
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| S7650 |
Peficitinib (ASP015K)Peficitinib (ASP015K, JNJ-54781532)是一种口服具有生物活性的 JAK 抑制剂。Phase 3。 |
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| S0871 |
Gusacitinib (ASN-002)Gusacitinib (ASN-002) 是一种新型有效的脾酪氨酸激酶 (SYK) 和 Janus 激酶 (JAK) 双重抑制剂，在生化试验中 IC50 值为 5-46 nM。 |
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| S0981 |
BD750BD750 是一种免疫抑制剂，同时也是 JAK3 和 STAT5 的双重抑制剂，可抑制IL-2诱导的JAK3/STAT5依赖性的T细胞增殖，影响小鼠和人T细胞增殖对应的IC50值分别为1.5 μM和1.1 μM。 |
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| S5904 |
WHI-P97WHI-P97是一种有效的JAK-3抑制剂，Ki值为0.09 μM，在EGFR激酶抑制试验中IC50为2.5 μM。 |
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| S7605 |
Filgotinib (GLPG0634)Filgotinib (GLPG0634)是一个选择性JAK1抑制剂，其对JAK1, JAK2, JAK3,和TYK2的IC50分别为10 nM, 28 nM, 810 nM,和116 nM。Phase 2。 |
Confocal microscopy showing BAFF in ductal epithelial structures within SG organoids from patients with sicca (Sc) or primary Sjögren's syndrome (SS). Nuclei were stained with DAPI (blue). Original magnification × 100.
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| S5903 |
JANEX-1JANEX-1 (WHI-P131)是JAK3小分子抑制剂，选择性抑制JAK3，IC50为78 μM。它不影响JAK1或JAK2，及其他蛋白酪氨酸激酶的活性（IC50 ≥ 350 µM）。 |
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| S7541 |
Decernotinib (VX-509)Decernotinib (VX-509)是一种有效的且选择性的JAK3抑制剂，Ki 为 2.5 nM，分别比作用于JAK1，JAK2，和 TYK2的选择性高4倍以上。Phase 2/3。 |
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| S5754 |
Baricitinib phosphateBaricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. |
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| S7144 |
BMS-911543BMS-911543是一种有效的、选择性JAK2小分子抑制剂，IC50为1.1 nM。 |
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| S7259 |
FLLL32FLLL32 是一种有效的 JAK2/STAT3 抑制剂，IC50 <5 μM。FLLL32 在乳腺癌细胞中通过 IFNα 和 IL-6 来抑制STAT3磷酸化的诱导。 |
Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.
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| S6919 |
Brevilin ABrevilin A (6-O-Angeloylplenolina) 是一种从Centipeda minima分离得到的倍半萜内酯，是 STAT3 的选择性抑制剂，可通过阻断JAKs酪氨酸激酶结构域 JH1 来减弱 JAKs 的活性。Brevilin A 可通过线粒体途径和 PI3K/AKT/mTOR 失活来诱导结肠腺癌细胞CT26的凋亡和自噬。 |
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| S5902 |
1,2,3,4,5,6-Hexabromocyclohexane1,2,3,4,5,6-Hexabromocyclohexane (NSC7908)是一种有效的JAK2酪氨酸激酶自身磷酸化抑制剂，IC50在较低的微摩尔级范围。 |
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| S8804 |
Brepocitinib (PF-06700841)Brepocitinib (PF-06700841, PF-841)是一种有效的Tyk2和Jak1抑制剂，对Tyk2, Jak1和Jak2的IC50分别为23 nM, 17 nM和77 nM。 |
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| S2407 |
CurcumolCurcumol是常见的传统中药，具有抗肿瘤活性。 |
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| S5917 |
SolcitinibSolcitinib (GLPG0778, GSK2586184) 是JAK1抑制剂，IC50为8-9 nM，对JAK2、JAK3和TYK2的IC50分别是JAK1的IC50的11倍、55倍和23倍。 |
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| S0374 |
GDC046GDC046 (Compound 3) 是一种有效的、选择性的 TYK2 的口服生物利用抑制剂，对TYK2、JAK1、JAK2和JAK3的Ki值分别为4.8 nM、83.8 nM、27.6 nM和253 nM。 |
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| S7137 |
GLPG0634 analogueGLPG0634 analogue 是选择性的JAK1抑制剂，其作用于JAK1, JAK2, JAK3, 和 TYK2 的IC50分别为10 nM, 28 nM, 810 nM, 和 116 nM 。Phase 2。 |
Western blots showing the expression of γ-globin after treatments with (F) GLPG0634.
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| S0384 |
RO495RO495 (CS-2667) 是一种 Non-receptor tyrosine-protein kinase 2 (TYK2) 的有效抑制剂。 |
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| S3566 |
Cerdulatinib (PRT062070)Cerdulatinib (PRT-062070, PRT2070) 是一种具有口服活性的多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶，IC50均低于200 nM。 |
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| S8195 |
Oclacitinib maleateOclacitinib maleate (PF-03394197)是一种新型的JAK family members以及JAK1-dependent cytokines抑制剂，IC50分别为10-99 nM(JAK family members)和36-249 nM(JAK1-dependent cytokines)。 |
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| S0391 |
TG-89TG-89 是 JAK2 的抑制剂，其IC50值为11.2 μM. |
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| S7634 |
Cerdulatinib (PRT062070) hydrochlorideCerdulatinib (PRT-062070, PRT2070) hydrochloride 是一种具有口服活性的多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶，IC50均低于200 nM。 |
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| S9676 |
Ropsacitinib (PF-06826647)Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) 是一种选择性的 tyrosine kinase 2 (TYK2) 的口服抑制剂，IC50值为17 nM，可与TYK2催化活性JH1结构域结合。PF-06826647 (Tyk2-IN-8, compound 10) 也可抑制 JAK1 和 JAK2，对应的IC50值分别为383 nM和74 nM。PF-06826647 (Tyk2-IN-8, compound 10) 可用于治疗牛皮癣(PSO)。 |
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| S5588 |
CreatineCreatine (Methylguanidoacetic acid) 是一种天然存在于脊椎动物中的含氮有机酸。Creatine 可以通过抑制 IFN-γ receptors 与 JAK2 的相互作用来抑制 JAK-STAT1 信号传递，以ATP非依赖性的方式促进三磷酸腺苷（ATP）的循环，从而抑制下游促炎基因表达。 |
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| S8541 |
FM-381FM-381是JAK3的特异性抑制剂，抑制作用具有可逆性，与JAK3共价结合，IC50为127 pM。对JAK3的选择性分别是对JAK1、JAK2、TYK2的400倍、2700倍、3600倍。 |
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| S0437 |
SAR-20347SAR-20347 是一种有效的 TYK2、JAK1、JAK2 和 JAK3 的抑制剂，对应的IC50值为0.6 nM、23 nM、26 nM和41 nM。SAR-20347可抑制TYK2和JAK1介导的 IL-12 和 IFN-α 信号传导。 |
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| S8879 |
Deucravacitinib (BMS-986165)Deucravacitinib (BMS-986165)是一种强效的、选择性的 Tyk2 的变构抑制剂，其与 Tyk2 假激酶结构域结合的Ki值为0.02 nM。它对一组265种激酶和假激酶的实验中具有高度的选择性。 |
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| S7812 |
Itacitinib (INCB39110)Itacitinib (INCB39110)是Janus-associated kinase 1 (JAK1)的抑制剂，具有口服生物活性和潜在的抗肿瘤活性。 |
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| S7119 |
Go6976Go6976 (PD406976)是一种强效的PKC抑制剂，其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM，2.3 nM, 和 6.2 nM 。此外，也是JAK2 和 Flt3的强抑制剂。 |
Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots. |
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| S8684 |
Selective JAK3 inhibitor 1Selective JAK3 inhibitor 1是一种不可逆的JAK3抑制剂，对JAK3、JAK1和JAK2的Ki值分别为0.07 nM、320 nM和740 nM。它对JAK3的选择性比对BMX、EGFR、ITK和BTK高。 |
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| S8765 |
Abrocitinib (PF-04965842)Abrocitinib (PF-04965842) 是一种有效的JAK1抑制剂，对JAK1、JAK2、JAK3和TYK2的IC50值分别为29 nM、803 nM、>10000 nM和1250 nM。 |
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| S8162 |
Upadacitinib (ABT-494)Upadacitinib (ABT-494)是选择性JAK1抑制剂，对JAK1和JAK2的IC50值分别为0.045 μM和0.109 μM，而对JAK3和TYK2的IC50值分别为2.1 μM和4.7 μM。 |
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| E2032New |
MOTS-cMOTS-c是一种线粒体来源的多肽(MDP)，通过激活AMPK通路，抑制MAP激酶-c-fos信号通路发挥抗伤害和抗炎作用。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1378 |
Ruxolitinib (INCB018424)Ruxolitinib (INCB018424)是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1， JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。 |
STAT3 phosphorylation as determined by phospho flow, mixed lymphocyte reactions containing BALB/c spleen-derived CD4+ T cells co-cultured with or without C57BL/6 BM-derived DC preactivated with 20 ng/mL LPS.
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| S5001 |
Tofacitinib (CP-690550) CitrateTofacitinib citrate (CP-690550, Tasocitinib)是一种新型JAK抑制剂，对JAK3，JAK2，JAK1的IC50分别为1 nM, 20 nM 和112 nM。Tofacitinib citrate 还具有抗感染的活性。 |
CP-690550 reduced the severity of ischemic damage. (A) CP-690550 (10 μM) suppressed IL-17 production by cdT cells and activated memory T cells. cdT cells and CD4+ CD44+ memory T cells isolated from C5BL6J mice through flow cytometry were stimulated for 24 h with plate-bound monoclonal antibodies to CD3 (2 ng/ml) and CD28 (1 ng/ml) in the presence or absence of IL-23 (25 ng/ml). IL-17A production and IL-17A expression level were measured by quantitative RT-PCR (a) and ELISA (b). (B) CBF reduction after brain ischemia. (C) Time-dependent changes in neurological score. *p < 0.05. (D) Infarct volume as visualized through TTC staining on day 3 in CP-690550 (CP)- and vehicle-treated mice.
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| S2162 |
AZD1480AZD1480是一种新型，ATP竞争性的JAK2抑制剂，无细胞试验中IC50为0.26 nM，选择性作用于JAK3和Tyk2，对JAK1的作用较弱。Phase 1。 |
HEL cells were treated for 3 hours with the indicated concentrations of AZD1480. AZD1480 inhibits Jak2-V617F mediated signal transduction at micromolar concentrations in intact cells.
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| S2736 |
Fedratinib (TG101348)Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3) 和 Ret (c-RET)，对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。 |
Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.
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| S1134 |
AT9283AT9283是一种有效的JAK2/3抑制剂，无细胞试验中IC50为1.2 nM/1.1 nM；对Aurora A/B，Abl1(T315I)也有效。Phase 2。 |
HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
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| E0933New |
AristolactamAristolactam (Aristolactam I) is the main active ingredient in the Aristolochia plant species, which have been associated with severe nephrotoxicity. |
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| S7002New |
ZotiraciclibZotiraciclib (SB1317; TG02)是一种新型小分子CDK/JAK2/FLT3抑制剂，对CDK1、2和9的IC50分别为9、5和3 nM，抑制FLT3的IC50为19 nM，抑制JAK2的IC50为19 nM。 |
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| S8152New |
Cucurbitacin ICucurbitacin-I (Elatericin B, JSI 124, NSC 521777)，一种从葫芦科植物中分离出来的天然细胞渗透性三萜，是一种新型的 JAK2/STAT3 选择性抑制剂。 |
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| S6789New |
JAK Inhibitor I (Pyridone 6)JAK Inhibitor I (Pyridone 6, CMP 6, Compound 6) 是一种泛 JAK 抑制剂，对JAK2, TYK2, JAK3 和 JAK1 的IC50分别为 1 nM, 1 nM, 5 nM 和 15 nM。 |
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| E0011New |
LinderalactoneLinderalactone 通过调节 A-549 细胞中 凋亡相关蛋白（Bax 和 Bcl-2） 的表达来抑制人肺癌的生长，IC50 为 15 µM。Linderalactone 诱导 G2/M 细胞周期停滞，还可以抑制 JAK/STAT 信号通路。Linderalactone 可以从 Radix linderae 中分离出来。 |
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| S1143 |
AG-490 (Tyrphostin B42)AG-490 (Tyrphostin B42, Zinc02557947) 是一种EGFR抑制剂，在无细胞试验中IC50为0.1 μM，作用于EGFR比作用于ErbB2选择性高135倍，对JAK2也有抑制作用，对Lck，Lyn，Btk，Syk和Src没有抑制活性。 |
Inhibition of JAK1/2 with AG490 or STAT3 with S3I-201 leads to reduced STAT3 activation and reduced WASF3 levels. In contrast, treatment with Dasatinib (SRC inhibitor) or Gefitinib (EGFR inhibitor) does not significantly affect activated STAT3 or WASF3 levels
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| S2219 |
Momelotinib (CYT387)Momelotinib (CYT387, LM-1149 , CYT11387) 是一种ATP竞争性JAK1/JAK2抑制剂，IC50为11 nM/18 nM，比作用于JAK3选择性约高10倍左右。Momelotinib (CYT387) 可诱导凋亡和自噬。Phase 3。 |
IL-6- supported INA-6 cells were treated with the JAK inhibitors ruxolitinib (Rux; 10 nM) or CYT387 (CYT; 50 nM) for 1 hour and assessed for inhibition of STAT3 phosphorylation by immunoblotting.
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| S2789 |
Tofacitinib (CP-690550)Tofacitinib (CP-690550,Tasocitinib)是一种新型JAK3抑制剂，在无细胞试验中IC50为1 nM，作用于JAK2和JAK1选择性低20到100倍。Tofacitinib 可在人类浆细胞样树突状细胞PDC中抑制抗凋亡的BCL-A1和BCL-XL并诱导PDC凋亡。 |
TRAP-positive multinucleated cell differentiation depends on JAK and is inhibited by tofacitinib in vitro. Effect of tofacitinib on the differentiation of TRAP-positive multi-nucleated cells in vitro (n =3 wells/experiment). Original magnification x 100.
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| S2796 |
WP1066WP1066 是一种新型JAK2和STAT3抑制剂，在HEL细胞中IC50分别为2.30 μM和2.43 μM；对JAK2，STAT3，STAT5和ERK1/2具有抑制活性，而对JAK1和JAK3没有作用。WP1066 可诱导凋亡。Phase 1。 |
Effects of selective STAT3 inhibitors on adherent glioma CSCs. Cells were treated with WP1066 (50 uM for 2 h) or vehicle, and colocalization of STAT3 and p65 was determined by immunostaining.
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| S2692 |
TG101209TG101209是一种选择性的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET (c-RET)作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。 |
EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (*,P < 0.05; **, P < 0.01; ***, P < 0.001; NS, nonsignificant).
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| S2179 |
Gandotinib (LY2784544)Gandotinib (LY2784544)是一种有效的JAK2抑制剂，IC50为3 nM，作用于JAK2V617F有效，比作用于JAK1和JAK3选择性高8和20倍。Phase 2。 |
HEL cells were treated for 3 hours with the indicated concentrations of LY2784544. LY2784544 inhibits Jak2-V617F mediated signal transduction at submicromolar concentrations in intact cells.
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| S2686 |
NVP-BSK805 2HClNVP-BSK805 2HCl是一种有效的，选择性的，ATP竞争性的JAK2抑制剂，IC50为0.5 nM，比作用于JAK1， JAK3和TYK2选择性高20倍以上。 |
Determination of the kynurenine production in HFF cells after IDO induction by IFN-γ (100 U/mL). The cells were incubated for 72 h under normoxia (20% O2) or hypoxia (1% O2) and treated with different amounts of the JAK2 inhibitor BSK805 (0-2 uM).
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| S2851 |
Baricitinib (INCB028050)Baricitinib (LY3009104, INCB028050)是一种选择性JAK1和JAK2抑制剂，无细胞试验中IC50分别为5.9 nM和5.7 nM，比作用于JAK3和Tyk2选择性高70和10倍左右，对c-Met和Chk2没有抑制作用。Baricitinib被发现可以减少或干扰病毒进入目标细胞，并用于COVID-19的治疗研究中。Phase 3 |
bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test. |
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| S2214 |
AZ 960AZ 960 是一种新型的，ATP竞争性的JAK2抑制剂，IC50和Ki分别低于3 nM和0.45 nM，作用于JAK2比作用于JAK3选择性高3倍。AZ 960 可诱导凋亡和生长阻滞。 |
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| S2806 |
CEP-33779CEP-33779是一种选择性JAK2抑制剂，IC50为1.8 nM，比作用于JAK1和TYK2选择性高40多倍和800多倍。 |
Potentiation of the antitumor effects of vincristine by CEP-33779 in a KBv200 cell xenograft model in nude mice. (A) The changes in tumor volume with time after tumor cell implantation. (B) The photograph of tumor size was taken on the 21st day after implantation. The various treatments were as follows: (a) Control (vehicle alone); (b) Vincristine (q2d x 6, ip, 0.2 mg/kg); (c) CEP-33779 (q2d x 6, p.o, 30 mg/kg) and (d) Vincristine (q2d x 6, ip, 0.2 mg/kg) plus CEP-33779 (q2d ?6, p.o, 30 mg/kg, given an hour before Vincristine administration).
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| S8057 |
Pacritinib (SB1518)Pacritinib (SB1518)是有效的选择性Janus Kinase 2 (JAK2)和Fms-Like Tyrosine Kinase-3 (FLT3)抑制剂，无细胞试验中IC50分别为23和22 nM。Phase 3。 |
Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting
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| S2867 |
WHI-P154WHI-P154是一种有效的JAK3抑制剂，IC50为1.8 μM，对JAK1和JAK2没有抑制活性，也抑制EGFR， Src， Abl， VEGFR和MAPK，抑制Stat3而非Stat5磷酸化。 |
Reversal effect of WHI-P154 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without WHI-P154. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line. |
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| S7198 |
BIOBIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052)是一种特异性的GSK-3抑制剂，无细胞试验中作用于GSK-3α/β的IC50为5 nM，比作用于CDK5选择性高16倍以上，也是一种泛JAK抑制剂，对 Tyk2 的IC50值为30 nM。BIO 可在人类黑色素瘤细胞中诱导凋亡。 |
Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.
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| S7036 |
XL019XL019是一种有效的，选择性的JAK2抑制剂，IC50为2.2 nM，比作用于JAK1， JAK3和TYK2.选择性高50倍。Phase 1。 |
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| S2902 |
S-Ruxolitinib (INCB018424)S-Ruxolitinib (INCB018424)是第一个应用到临床的，有效的，选择性JAK1/2抑制剂，IC50为3.3 nM/2.8 nM，作用于JAK1/2比作用于JAK3选择性高130倍以上。 Phase 3。 |
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| S8004 |
ZM 39923 HClZM 39923 HCl是一种JAK1/3抑制剂，pIC50为4.4/7.1，对JAK2没有作用活性，适度有效作用于EFGR；对转谷氨酰胺酶敏感。 |
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| S6899 |
Licochalcone DLicochalcone D (Lico D, LCD, LD) 是一种从中草药甘草 Glycyrrhiza inflata 中分离出的类黄酮，具有抗氧化、抗炎和抗癌的特性。Licochalcone D 可抑制LPS信号通路中NF-κB p65的磷酸化。Licochalcone D 可抑制 JAK2、EGFR 和 Met (c-Met) 活性，并诱导ROS依赖性的凋亡。Licochalcone D 还可诱导 caspases 的活化和 poly (ADP-ribose) polymerase (PARP) 的裂解。 |
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| S6521 |
WHI-P258WHI-P258是JAK3的抑制剂，Ki值为72 μM。 |
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| S0918 |
Ginkgolic acid C17:1Ginkgolic acid C17:1 (GAC 17:1) 通过废除上游的 JAK2 和 Src 来抑制 STAT3 的组成性激活。Ginkgolic acid C17:1 可以诱导 PTEN 和 SHP-1 的大量表达。Ginkgolic acid C17:1 诱导肿瘤细胞凋亡。 |
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| S3267 |
Kaempferol-3-O-rutinosideKaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside) 是从 Carthamus tinctorius 中提取的黄酮，可改变受伤神经元的形状和结构，减少凋亡细胞，下调 p-JAK2、p-STAT3、caspase-3 和 Bax 的表达，并降低Bax免疫反应性，并增加 Bcl-2 蛋白表达和免疫反应性。 |
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| S8538 |
Ritlecitinib (PF-06651600)Ritlecitinib (PF-06651600)是JAK3选择性的抑制剂，IC50为33.1 nM。对JAK1、JAK2和TYK2没有活性(IC50 > 10 000 nM)。 |
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| S5554 |
Lanatoside CLanatoside C 是具有抗病毒和抗肿瘤活性的强心苷。Lanatoside C 通过减弱 MAPK，Wnt，JAK-STAT和PI3K/AKT/mTOR信号通路，诱导G2/M细胞周期停滞并诱导自噬和细胞凋亡。 |
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| S5243 |
Ruxolitinib PhosphateRuxolitinib Phosphate (INCB018424, INC424)是Ruxolitinib的磷酸盐形式。Ruxolitinib 是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1，JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。 |
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| S6524 |
NSC 42834NSC42834 (JAK2 Inhibitor V, Z3)是野生型JAK2和JAK2(V617F)自身磷酸化的抑制剂，IC50的范围为10-30 μM。 |
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| S7650 |
Peficitinib (ASP015K)Peficitinib (ASP015K, JNJ-54781532)是一种口服具有生物活性的 JAK 抑制剂。Phase 3。 |
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| S0871 |
Gusacitinib (ASN-002)Gusacitinib (ASN-002) 是一种新型有效的脾酪氨酸激酶 (SYK) 和 Janus 激酶 (JAK) 双重抑制剂，在生化试验中 IC50 值为 5-46 nM。 |
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| S0981 |
BD750BD750 是一种免疫抑制剂，同时也是 JAK3 和 STAT5 的双重抑制剂，可抑制IL-2诱导的JAK3/STAT5依赖性的T细胞增殖，影响小鼠和人T细胞增殖对应的IC50值分别为1.5 μM和1.1 μM。 |
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| S5904 |
WHI-P97WHI-P97是一种有效的JAK-3抑制剂，Ki值为0.09 μM，在EGFR激酶抑制试验中IC50为2.5 μM。 |
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| S7605 |
Filgotinib (GLPG0634)Filgotinib (GLPG0634)是一个选择性JAK1抑制剂，其对JAK1, JAK2, JAK3,和TYK2的IC50分别为10 nM, 28 nM, 810 nM,和116 nM。Phase 2。 |
Confocal microscopy showing BAFF in ductal epithelial structures within SG organoids from patients with sicca (Sc) or primary Sjögren's syndrome (SS). Nuclei were stained with DAPI (blue). Original magnification × 100.
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| S5903 |
JANEX-1JANEX-1 (WHI-P131)是JAK3小分子抑制剂，选择性抑制JAK3，IC50为78 μM。它不影响JAK1或JAK2，及其他蛋白酪氨酸激酶的活性（IC50 ≥ 350 µM）。 |
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| S7541 |
Decernotinib (VX-509)Decernotinib (VX-509)是一种有效的且选择性的JAK3抑制剂，Ki 为 2.5 nM，分别比作用于JAK1，JAK2，和 TYK2的选择性高4倍以上。Phase 2/3。 |
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| S5754 |
Baricitinib phosphateBaricitinib phosphate (INCB-028050, LY-3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. |
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| S7144 |
BMS-911543BMS-911543是一种有效的、选择性JAK2小分子抑制剂，IC50为1.1 nM。 |
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| S7259 |
FLLL32FLLL32 是一种有效的 JAK2/STAT3 抑制剂，IC50 <5 μM。FLLL32 在乳腺癌细胞中通过 IFNα 和 IL-6 来抑制STAT3磷酸化的诱导。 |
Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.
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| S6919 |
Brevilin ABrevilin A (6-O-Angeloylplenolina) 是一种从Centipeda minima分离得到的倍半萜内酯，是 STAT3 的选择性抑制剂，可通过阻断JAKs酪氨酸激酶结构域 JH1 来减弱 JAKs 的活性。Brevilin A 可通过线粒体途径和 PI3K/AKT/mTOR 失活来诱导结肠腺癌细胞CT26的凋亡和自噬。 |
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| S5902 |
1,2,3,4,5,6-Hexabromocyclohexane1,2,3,4,5,6-Hexabromocyclohexane (NSC7908)是一种有效的JAK2酪氨酸激酶自身磷酸化抑制剂，IC50在较低的微摩尔级范围。 |
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| S8804 |
Brepocitinib (PF-06700841)Brepocitinib (PF-06700841, PF-841)是一种有效的Tyk2和Jak1抑制剂，对Tyk2, Jak1和Jak2的IC50分别为23 nM, 17 nM和77 nM。 |
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| S2407 |
CurcumolCurcumol是常见的传统中药，具有抗肿瘤活性。 |
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| S5917 |
SolcitinibSolcitinib (GLPG0778, GSK2586184) 是JAK1抑制剂，IC50为8-9 nM，对JAK2、JAK3和TYK2的IC50分别是JAK1的IC50的11倍、55倍和23倍。 |
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| S0374 |
GDC046GDC046 (Compound 3) 是一种有效的、选择性的 TYK2 的口服生物利用抑制剂，对TYK2、JAK1、JAK2和JAK3的Ki值分别为4.8 nM、83.8 nM、27.6 nM和253 nM。 |
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| S7137 |
GLPG0634 analogueGLPG0634 analogue 是选择性的JAK1抑制剂，其作用于JAK1, JAK2, JAK3, 和 TYK2 的IC50分别为10 nM, 28 nM, 810 nM, 和 116 nM 。Phase 2。 |
Western blots showing the expression of γ-globin after treatments with (F) GLPG0634.
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| S0384 |
RO495RO495 (CS-2667) 是一种 Non-receptor tyrosine-protein kinase 2 (TYK2) 的有效抑制剂。 |
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| S3566 |
Cerdulatinib (PRT062070)Cerdulatinib (PRT-062070, PRT2070) 是一种具有口服活性的多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶，IC50均低于200 nM。 |
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| S8195 |
Oclacitinib maleateOclacitinib maleate (PF-03394197)是一种新型的JAK family members以及JAK1-dependent cytokines抑制剂，IC50分别为10-99 nM(JAK family members)和36-249 nM(JAK1-dependent cytokines)。 |
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| S0391 |
TG-89TG-89 是 JAK2 的抑制剂，其IC50值为11.2 μM. |
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| S7634 |
Cerdulatinib (PRT062070) hydrochlorideCerdulatinib (PRT-062070, PRT2070) hydrochloride 是一种具有口服活性的多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。也能够抑制测试的其他19种激酶，IC50均低于200 nM。 |
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| S9676 |
Ropsacitinib (PF-06826647)Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) 是一种选择性的 tyrosine kinase 2 (TYK2) 的口服抑制剂，IC50值为17 nM，可与TYK2催化活性JH1结构域结合。PF-06826647 (Tyk2-IN-8, compound 10) 也可抑制 JAK1 和 JAK2，对应的IC50值分别为383 nM和74 nM。PF-06826647 (Tyk2-IN-8, compound 10) 可用于治疗牛皮癣(PSO)。 |
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| S5588 |
CreatineCreatine (Methylguanidoacetic acid) 是一种天然存在于脊椎动物中的含氮有机酸。Creatine 可以通过抑制 IFN-γ receptors 与 JAK2 的相互作用来抑制 JAK-STAT1 信号传递，以ATP非依赖性的方式促进三磷酸腺苷（ATP）的循环，从而抑制下游促炎基因表达。 |
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| S8541 |
FM-381FM-381是JAK3的特异性抑制剂，抑制作用具有可逆性，与JAK3共价结合，IC50为127 pM。对JAK3的选择性分别是对JAK1、JAK2、TYK2的400倍、2700倍、3600倍。 |
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| S0437 |
SAR-20347SAR-20347 是一种有效的 TYK2、JAK1、JAK2 和 JAK3 的抑制剂，对应的IC50值为0.6 nM、23 nM、26 nM和41 nM。SAR-20347可抑制TYK2和JAK1介导的 IL-12 和 IFN-α 信号传导。 |
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| S8879 |
Deucravacitinib (BMS-986165)Deucravacitinib (BMS-986165)是一种强效的、选择性的 Tyk2 的变构抑制剂，其与 Tyk2 假激酶结构域结合的Ki值为0.02 nM。它对一组265种激酶和假激酶的实验中具有高度的选择性。 |
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| S7812 |
Itacitinib (INCB39110)Itacitinib (INCB39110)是Janus-associated kinase 1 (JAK1)的抑制剂，具有口服生物活性和潜在的抗肿瘤活性。 |
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| S7119 |
Go6976Go6976 (PD406976)是一种强效的PKC抑制剂，其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM，2.3 nM, 和 6.2 nM 。此外，也是JAK2 和 Flt3的强抑制剂。 |
Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots. |
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| S8684 |
Selective JAK3 inhibitor 1Selective JAK3 inhibitor 1是一种不可逆的JAK3抑制剂，对JAK3、JAK1和JAK2的Ki值分别为0.07 nM、320 nM和740 nM。它对JAK3的选择性比对BMX、EGFR、ITK和BTK高。 |
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| S8765 |
Abrocitinib (PF-04965842)Abrocitinib (PF-04965842) 是一种有效的JAK1抑制剂，对JAK1、JAK2、JAK3和TYK2的IC50值分别为29 nM、803 nM、>10000 nM和1250 nM。 |
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| S8162 |
Upadacitinib (ABT-494)Upadacitinib (ABT-494)是选择性JAK1抑制剂，对JAK1和JAK2的IC50值分别为0.045 μM和0.109 μM，而对JAK3和TYK2的IC50值分别为2.1 μM和4.7 μM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| E2032New |
MOTS-cMOTS-c是一种线粒体来源的多肽(MDP)，通过激活AMPK通路，抑制MAP激酶-c-fos信号通路发挥抗伤害和抗炎作用。 |
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