JAK

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抑制剂选择性比较

特异性亚型抑制剂

JAK产品

所有产品 JAK抑制剂(44) 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 Med, 2019, 25(1):95-102 Cancer Discov, 2019, 9(1):34-45 Cell Stem Cell, 2019, 25(1):69-86	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.
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。	Nat Immunol, 2019, 20(2):152-162 Gastroenterology, 2019, 157(5):1310-1322 Haematologica, 2019, 10.3324/haematol.2018.212126	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。	Cell Stem Cell, 2019, 25(1):69-86 Nat Commun, 2019, 10(1):716 Nat Commun, 2019, 10(1):3601	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.
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。	Nat Cell Biol, 2019, 21(6):778-790 Haematologica, 2019, 10.3324/haematol.2018.212126 FASEB J, 2019, 10.1096/fj.201900215RR	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。	J Clin Invest, 2018, 128(1):387-401 Nat Commun, 2018, 9(1):358 Mol Cancer Ther, 2016, 15(2):334-42	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.
S8162^New	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。
S6524^New	NSC 42834 NSC42834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。
S6521^New	WHI-P258 WHI-P258是JAK3的抑制剂，Ki值为72 μM。
S8684^New	Selective JAK3 inhibitor 1 Selective 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。
S8804^New	PF-06700841 PF-06700841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。
S8765^New	PF-04965842 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。	Cell Death Dis, 2019, 10(4):319
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。	EMBO Rep, 2019, 20(10):e47734 Cancer Res, 2019, 79(20):5382-5393 Int Immunopharmacol, 2019, 73:482-490	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.
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。	Nat Commun, 2019, 10(1):4353 J Thromb Haemost, 2019, 10.1111/jth.14525 Pharmacol Res, 2019, 143:73-85	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.
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。	Haematologica, 2019, 10.3324/haematol.2018.203430 Redox Biol, 2019, 24:101189 Glia, 2019, 67(2):321-331	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.
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。	Nat Commun, 2018, 9(1):3259 Int Immunopharmacol, 2018, 54:354-365 Nat Commun, 2017, 8(1):1130	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。	J Thromb Haemost, 2019, 10.1111/jth.14525 Biochem Biophys Res Commun, 2018, 498(1):164-170 Cell Chem Biol, 2017, 24(7):858-869	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.
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。	BMC Cancer, 2019, 19(1):936 J Biol Chem, 2015, 290(39):23553-62 Cancer Lett, 2013, 341(2):224-30	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。	Exp Mol Med, 2019, 51(7):75 Cell Commun Signal, 2019, 17(1):46 Nephron, 2019, 10.1159/000499506	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。	Nat Commun, 2019, 10(1):716 Cytokine, 2019, 113:238-247 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。	Sci Rep, 2018, 8(1):15645 Biosci Rep, 2017, 37(4) Anticancer Res, 2017, 37(12):6761-6769	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。	Exp Cell Res, 2019, 378(1):11-20 Clin Cancer Res, 2016, 22(24):6118-6128	Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting
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。	Biol Open, 2018, 7(1) J Mol Med, 2018, 10.1007/s00109-018-1724-8 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。	Anticancer Res, 2017, 37(12):6761-6769
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。	Blood Cancer J, 2017, 7(6):e572 Nature, 2017, 548(7668):471-475 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。	Cancer Sci, 2018, 109(12):3726-3736 Oncoimmunology, 2017, 6(11):e1353860
S8538	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)。
S5243	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.	Front Immunol, 2019, 10:1659 Cell Commun Signal, 2019, 17(1):46 Int J Mol Sci, 2019, 20(13)
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。
S5904	WHI-P97 WHI-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。
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。	Gastroenterology, 2019, 157(5):1310-1322 Cancer Immunol Res, 2019, 7(5):813-827 Front Immunol, 2019, 10:1659	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.
S5903	JANEX-1 JANEX-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）。
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。
S5754	Baricitinib phosphate Baricitinib 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.	Arthritis Rheumatol, 2019, 71(1):50-62 Exp Mol Med, 2019, 51(7):75 Cell Commun Signal, 2019, 17(1):46
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。	Oncogene, 2019, 38(9):1477-1488 J Pathol, 2019, 10.1002/path.5280 Cancer Sci, 2018, 109(12):3726-3736
S7259	FLLL32 FLLL32是一种有效的 JAK2/STAT3 抑制剂，IC50 <5 μM。	Exp Ther Med, 2017, 14(4):3926-3934 Eur Rev Med Pharmacol Sci, 2017, 21(13):3005-3011 Cancer Sci, 2016, 107(7):944-54	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.
S5902	1,2,3,4,5,6-Hexabromocyclohexane 1,2,3,4,5,6-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。	Cell Tissue Res, 2016, 364(2):395-404
S2407	Curcumol Curcumol是常见的传统中药，具有抗肿瘤活性。
S5917	Solcitinib Solcitinib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。
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。	Int J Oncol, 2018, 53(4):1681-1690 Diabetologia, 2018, 61(3):636-640 J Immunol, 2017, 198(12):4596-4606
S8541	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。	Commun Biol, 2020, 3:8
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。
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。	Oncogene, 2019, 38(1):120-139 EBioMedicine, 2019, 40:151-162 Acta Physiol, 2018, 223(3):e13055	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.

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 Med,2019, 25(1):95-102 Cancer Discov,2019, 9(1):34-45 Cell Stem Cell,2019, 25(1):69-86	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.
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。	Nat Immunol,2019, 20(2):152-162 Gastroenterology,2019, 157(5):1310-1322 Haematologica,2019, 10.3324/haematol.2018.212126	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。	Cell Stem Cell,2019, 25(1):69-86 Nat Commun,2019, 10(1):716 Nat Commun,2019, 10(1):3601	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.
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。	Nat Cell Biol,2019, 21(6):778-790 Haematologica,2019, 10.3324/haematol.2018.212126 FASEB J,2019, 10.1096/fj.201900215RR	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。	J Clin Invest,2018, 128(1):387-401 Nat Commun,2018, 9(1):358 Mol Cancer Ther,2016, 15(2):334-42	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.
S8162^New	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。
S6524^New	NSC 42834 NSC42834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。
S6521^New	WHI-P258 WHI-P258是JAK3的抑制剂，Ki值为72 μM。
S8684^New	Selective JAK3 inhibitor 1 Selective 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。
S8804^New	PF-06700841 PF-06700841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。
S8765^New	PF-04965842 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。	Cell Death Dis,2019, 10(4):319
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。	EMBO Rep,2019, 20(10):e47734 Cancer Res,2019, 79(20):5382-5393 Int Immunopharmacol,2019, 73:482-490	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.
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。	Nat Commun,2019, 10(1):4353 J Thromb Haemost,2019, 10.1111/jth.14525 Pharmacol Res,2019, 143:73-85	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.
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。	Haematologica,2019, 10.3324/haematol.2018.203430 Redox Biol,2019, 24:101189 Glia,2019, 67(2):321-331	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.
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。	Nat Commun,2018, 9(1):3259 Int Immunopharmacol,2018, 54:354-365 Nat Commun,2017, 8(1):1130	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。	J Thromb Haemost,2019, 10.1111/jth.14525 Biochem Biophys Res Commun,2018, 498(1):164-170 Cell Chem Biol,2017, 24(7):858-869	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.
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。	BMC Cancer,2019, 19(1):936 J Biol Chem,2015, 290(39):23553-62 Cancer Lett,2013, 341(2):224-30	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。	Exp Mol Med,2019, 51(7):75 Cell Commun Signal,2019, 17(1):46 Nephron,2019, 10.1159/000499506	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。	Nat Commun,2019, 10(1):716 Cytokine,2019, 113:238-247 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。	Sci Rep,2018, 8(1):15645 Biosci Rep,2017, 37(4) Anticancer Res,2017, 37(12):6761-6769	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。	Exp Cell Res,2019, 378(1):11-20 Clin Cancer Res,2016, 22(24):6118-6128	Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting
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。	Biol Open,2018, 7(1) J Mol Med,2018, 10.1007/s00109-018-1724-8 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。	Anticancer Res,2017, 37(12):6761-6769
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。	Blood Cancer J,2017, 7(6):e572 Nature,2017, 548(7668):471-475 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。	Cancer Sci,2018, 109(12):3726-3736 Oncoimmunology,2017, 6(11):e1353860
S8538	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)。
S5243	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.	Front Immunol,2019, 10:1659 Cell Commun Signal,2019, 17(1):46 Int J Mol Sci,2019, 20(13)
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。
S5904	WHI-P97 WHI-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。
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。	Gastroenterology,2019, 157(5):1310-1322 Cancer Immunol Res,2019, 7(5):813-827 Front Immunol,2019, 10:1659	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.
S5903	JANEX-1 JANEX-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）。
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。
S5754	Baricitinib phosphate Baricitinib 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.	Arthritis Rheumatol,2019, 71(1):50-62 Exp Mol Med,2019, 51(7):75 Cell Commun Signal,2019, 17(1):46
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。	Oncogene,2019, 38(9):1477-1488 J Pathol,2019, 10.1002/path.5280 Cancer Sci,2018, 109(12):3726-3736
S7259	FLLL32 FLLL32是一种有效的 JAK2/STAT3 抑制剂，IC50 <5 μM。	Exp Ther Med,2017, 14(4):3926-3934 Eur Rev Med Pharmacol Sci,2017, 21(13):3005-3011 Cancer Sci,2016, 107(7):944-54	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.
S5902	1,2,3,4,5,6-Hexabromocyclohexane 1,2,3,4,5,6-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。	Cell Tissue Res,2016, 364(2):395-404
S2407	Curcumol Curcumol是常见的传统中药，具有抗肿瘤活性。
S5917	Solcitinib Solcitinib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。
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。	Int J Oncol,2018, 53(4):1681-1690 Diabetologia,2018, 61(3):636-640 J Immunol,2017, 198(12):4596-4606
S8541	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。	Commun Biol,2020, 3:8
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。
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。	Oncogene,2019, 38(1):120-139 EBioMedicine,2019, 40:151-162 Acta Physiol,2018, 223(3):e13055	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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