JAK
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1378 | Ruxolitinib (INCB018424) | <1 mg/mL | 61 mg/mL | 61 mg/mL |
| S5001 | Tofacitinib (CP-690550) Citrate | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2162 | AZD1480 | <1 mg/mL | 69 mg/mL | <1 mg/mL |
| S2736 | Fedratinib (SAR302503, TG101348) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1134 | AT9283 | <1 mg/mL | 76 mg/mL | 38 mg/mL |
| S5902 | 1,2,3,4,5,6-Hexabromocyclohexane | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S5903 | JANEX-1 | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S5904 | WHI-P97 | <1 mg/mL | 8 mg/mL | <1 mg/mL |
| S5754 | Baricitinib phosphate | -1 mg/mL | 94 mg/mL | -1 mg/mL |
| S5243 | Ruxolitinib Phosphate | 29 mg/mL | 80 mg/mL | 8 mg/mL |
| S7812 | Itacitinib (INCB39110) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S2219 | Momelotinib (CYT387) | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S2789 | Tofacitinib (CP-690550,Tasocitinib) | <1 mg/mL | 62 mg/mL | <1 mg/mL |
| S2796 | WP1066 | <1 mg/mL | 71 mg/mL | <1 mg/mL |
| S2692 | TG101209 | <1 mg/mL | 102 mg/mL | <1 mg/mL |
| S2179 | Gandotinib (LY2784544) | <1 mg/mL | 94 mg/mL | 9 mg/mL |
| S2686 | NVP-BSK805 2HCl | 3 mg/mL | 113 mg/mL | 15 mg/mL |
| S2851 | Baricitinib (LY3009104, INCB028050) | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S2214 | AZ 960 | <1 mg/mL | 71 mg/mL | 3 mg/mL |
| S2806 | CEP-33779 | <1 mg/mL | 36 mg/mL | <1 mg/mL |
| S8057 | Pacritinib (SB1518) | <1 mg/mL | 11 mg/mL | <1 mg/mL |
| S2867 | WHI-P154 | <1 mg/mL | 75 mg/mL | <1 mg/mL |
| S7036 | XL019 | <1 mg/mL | 16 mg/mL | <1 mg/mL |
| S2902 | S-Ruxolitinib (INCB018424) | 5 mg/mL | 61 mg/mL | 61 mg/mL |
| S8004 | ZM 39923 HCl | <1 mg/mL | 30 mg/mL | 8 mg/mL |
| S7650 | Peficitinib (ASP015K, JNJ-54781532) | <1 mg/mL | 65 mg/mL | <1 mg/mL |
| S7605 | Filgotinib (GLPG0634) | <1 mg/mL | 85 mg/mL | <1 mg/mL |
| S7541 | Decernotinib (VX-509) | <1 mg/mL | 78 mg/mL | 20 mg/mL |
| S7144 | BMS-911543 | <1 mg/mL | 36 mg/mL | 22 mg/mL |
| S7259 | FLLL32 | <1 mg/mL | 92 mg/mL | 25 mg/mL |
| S2407 | Curcumol | <1 mg/mL | 47 mg/mL | 47 mg/mL |
| S7137 | GLPG0634 analogue | <1 mg/mL | 0.1 mg/mL | <1 mg/mL |
| S8195 | Oclacitinib maleate | 18 mg/mL | 90 mg/mL | 90 mg/mL |
| S7634 | Cerdulatinib (PRT062070, PRT2070) | <1 mg/mL | 43 mg/mL | <1 mg/mL |
| S8541 | FM-381 | <1 mg/mL | 20 mg/mL | 2 mg/mL |
| S7119 | Go6976 | <1 mg/mL | 18 mg/mL | <1 mg/mL |
特异性亚型抑制剂
- JAK抑制剂（37）
- 新JAK产品
| 产品目录 | 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。 |
a, Phospho- and total STAT1 in MDA-MB-453 cells treated with abemaciclib with or without ruxolitinib for 7 days.
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| S5001 |
Tofacitinib (CP-690550) CitrateTofacitinib (CP-690550) Citrate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。 |
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。 |
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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| S2736 |
Fedratinib (SAR302503, 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。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，Abl(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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| S5902New |
1,2,3,4,5,6-Hexabromocyclohexane1,2,3,4,5,6-Hexabromocyclohexane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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| S5903New |
JANEX-1JANEX-1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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| S5904New |
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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| S5754New |
Baricitinib phosphateBaricitinib phosphate 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. |
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| S5243New |
Ruxolitinib PhosphateRuxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. |
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| S7812New |
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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| S8538New |
PF-06651600PF-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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| S2219 |
Momelotinib (CYT387)Momelotinib (CYT387)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。Phase 3。 |
Shown are WT pan T cells (both CD4＋and CD8＋ T cells; CD4－T cells are CD8＋T cells) after drug treatment. |
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| S2789 |
Tofacitinib (CP-690550,Tasocitinib)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。 |
(J) Western blotting analysis of HIF1α abundance in response to 100 nM tofacitinib. Quantification of HIF1α detected by Western blot is shown alongside, with data normalized to SMC1 intensity and HIF1α protein abundance in IL-2-maintained cytotoxic T lymphocytes.
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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。Phase 1。 |
BrdU assay for the proliferation of WP1066- treated UM1 and Tca8113 cells (P<0.05).
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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。 |
Relative expression of BCLXL, c-MYC, CCND1, MMP2 and VEGF in (A) HL60 cell line. Cells were treated with 1 µM of ruxolitinib, fedratinib, gandotinib or tofacitinib for 6 h. RE=1 for DMSO control. Asterix (*) denotes statistical significance (p<0.05). Error bars denotes±standard deviation. Each relative expression value was obtained from at least two biological experiments run in two technical repeats.
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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 (LY3009104, 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。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。 |
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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。 |
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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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| 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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| S7650 |
Peficitinib (ASP015K, JNJ-54781532)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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| 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。 |
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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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| 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。 |
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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| S2407 |
CurcumolCurcumol是常见的传统中药，具有抗肿瘤活性。 |
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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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| S8195 |
Oclacitinib maleateOclacitinib(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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| S7634 |
Cerdulatinib (PRT062070, PRT2070)Cerdulatinib (PRT-062070)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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| 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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| S7119 |
Go6976Go6976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。 |
Go6976 abolished the anticalcification activity of CST by promoting the ossification of cultured VSMCs. Rat VSMCs werecultured in growth medium or calcification medium in the presence or absence of 10 7mol/L of CST or in calcification medium containing10 7mol/L of CST and pretreated with different doses of Go6976 (0.01, 0.1 and 0.5lmol/L) for 30 min. On day 7 (A, n=4) and 12 (B,n=4), VSMCs were harvested for the determination of ALP activity (A) using an ALP assay kit and calcium content (B) using the OCPCmethod. The VSMCs cultured with calcification medium containing 10 7mol/L of CST were pretreated with different doses of Go6976 (0.01and 0.1lmol/L) for 30 min. On day 6, VSMCs were harvested for the detection of expression of OCN (C, D, n=6). Data from at least threeindependent experiments are presented as the mean SEM, and representative images are shown.*P<.05 and †P<.01. Ctrl, control groupin vitro;b-GP,b-glycerophosphate group;b-GP+CST,b-glycerophosphate plus 10 7mol/L cortistatin group;b-GP+CST+Go6976,b-glycerophosphate plus 10 7mol/L cortistatin plus Go6976 group.
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