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)
目录号	产品目录	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
S5243	Ruxolitinib Phosphate	29 mg/mL	80 mg/mL	8 mg/mL
S7812	Itacitinib (INCB39110)	<1 mg/mL	100 mg/mL	100 mg/mL
S8541	FM-381	<1 mg/mL	20 mg/mL	2 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
S7119	Go6976	<1 mg/mL	18 mg/mL	<1 mg/mL

特异性亚型抑制剂

JAK抑制剂（33）
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。	NAT MATER, 2017, 10.1038/NMAT5024 Nat Med, 2015, 10.1038/nm.4013 Cell, 2017, 171(1):217-228	a, Phospho- and total STAT1 in MDA-MB-453 cells treated with abemaciclib with or without ruxolitinib for 7 days.
S5001	Tofacitinib (CP-690550) Citrate Tofacitinib (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。	Cancer Discov, 2012, 2(7):591-7 Nat Cell Biol, 2015, 17(1):57-67 Blood, 2014, 124(5):761-70	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.
S2162	AZD1480 AZD1480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。	Nat Cell Biol, 2015, 17(1):57-67 Blood, 2014, 123(10):1516-24 Leukemia, 2012, 26(4):708-15	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.
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。	Cell, 2015, 162(2):441-51 Blood, 2014, 123(20):3175-84 J Thorac Oncol, 2016, 11(1):62-71	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.
S1134	AT9283 AT9283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。	Cell Stem Cell, 2012, 11(2):179-94 Cancer Res, 2013, 73(20):6310-22 Cancer Lett, 2013, 341(2):224-30	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.
S5243^New	Ruxolitinib Phosphate Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.
S7812^New	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。
S8538^New	PF-06651600 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)。
S8541^New	FM-381 FM-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。
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。	Nat Cell Biol, 2015, 17(1):57-67 Blood, 2012, 120(19):4093-103 J Clin Invest, 2014, 124(12):5263-74	Shown are WT pan T cells (both CD4＋and CD8＋ T cells; CD4－T cells are CD8＋T cells) after drug treatment.
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。	Blood, 2014, 124(5):761-70 Blood, 2011, 118(14):3911-21 Blood, 2012, 120(4):709-19	(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.
S2796	WP1066 WP1066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。	Clin Cancer Res, 2018, 24(11):2665-2677 Int J Cancer, 2014, 135(2):282-94 Exp Neurol, 2015, 271:445-56	(A) HRMECs were treated with IL-6 for 48 hours in the presence and the absence of WP1066. The protein expression and localization of ZO-1 was examined by immunofluorescence staining. Each tight junction protein was doubleimmunostained with anti-CD31 antibody for defining the cell boundaries. Nuclei were labeled with DAPI. Arrow heads indicate the intact tight junction protein at cell boundaries. Scale bars are equal to 50 μm. Right histograms: quantitative analysis of each tight junction protein expression by evaluating the fluorescence intensity using with ImageJ software. The results are fold increases versus control and plotted as the means ± SD (n = 5). * P < 0.05 between two values.
S2692	TG101209 TG101209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。	Leukemia, 2014, 28(7):1519-28 Cancer Lett, 2013, 341(2):224-30 ACS Chem Biol, 2014, 9(5):1160-71	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).
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。	Cancer Lett, 2013, 341(2):224-30 Gastric Cancer, 2016, 19(1):53-62 Eur J Pharmacol, 2015, 765:188-97	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.
S2686	NVP-BSK805 2HCl NVP-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。	Cancer Lett, 2013, 341(2):224-30 PLoS One, 2013, 8(5):e63301	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).
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。	Nat Cell Biol, 2014, 17(1):57-67 Br J Haematol, 2017, 177(2):271-282	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.
S2214	AZ 960 AZ 960是一种新型的，ATP竞争性的JAK2抑制剂，IC50和K_i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。	Cancer Lett, 2013, 341(2):224-30
S2806	CEP-33779 CEP-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。	Biochem Pharmacol, 2014, 91(2):144-56 Biosci Rep, 2017, 37(4)	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).
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。
S2867	WHI-P154 WHI-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。	Oncol Rep, 2017, 37(1):66-76	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.
S7036	XL019 XL019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。
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。	Clin Cancer Res, 2015, 21(16):3740-9 Blood Cancer J, 2017, 7(6):e572 Sci Rep, 2016, 6:28473
S8004	ZM 39923 HCl ZM 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。
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。
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。
S7541	Decernotinib (VX-509) Decernotinib (VX-509)是一种有效的且选择性的JAK3抑制剂，K_i 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。
S7144	BMS-911543 BMS-911543是一种有效的、选择性JAK2小分子抑制剂，IC50为1.1 nM。
S7259	FLLL32 FLLL32是一种有效的 JAK2/STAT3 抑制剂，IC50 <5 μM。	Cancer Sci, 2016, 107(7):944-54 Eur Rev Med Pharmacol Sci, 2017, 21(13):3005-3011	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.
S2407	Curcumol Curcumol是常见的传统中药，具有抗肿瘤活性。
S7137	GLPG0634 analogue GLPG0634 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.
S8195	Oclacitinib maleate Oclacitinib(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)。
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。	J Immunol, 2016, 197(7):2948-57
S7119	Go6976 Go6976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。	Cell Signal, 2016, 28(9):1422-31 Infect Immun, 2017, e00087-17	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.

研究领域

产品类型

JAK

信号通路图

研究领域

特异性亚型抑制剂