JAK
Catalog No. | Inhibitor Name | JAK1 | JAK2 | JAK3 | Tyk2 | Other |
---|---|---|---|---|---|---|
A11041 | Ruxolitinib | *** | **** | |||
A10241 | Tofacitinib Citrate | ** | ** | **** | ROCK2,LCK | |
A10110 | AZD1480 | **** | ||||
A11082 | Fedratinib | **** | FLT3,RET | |||
A10095 | AT9283 | **** | **** | *** | Aurora B,Aurora A,Abl1 | |
A10047 | AG-490 | * | EGFR,ErbB2 | |||
A10263 | Momelotinib | *** | *** | * | ||
A11795 | WP1066 | * | STAT3 | |||
A11180 | TG101209 | *** | * | RET,FLT3 | ||
A10546 | Gandotinib | ** | **** | ** | ** | FLT3,FLT4,FGFR2 |
A11193 | NVP-BSK805 2HCl | ** | **** | *** | *** | |
A11329 | Baricitinib | *** | *** | ** | ||
A10104 | AZ 960 | **** | ||||
A12808 | CEP-33779 | **** | ||||
A12694 | Pacritinib | * | ** | * | ** | FLT3 (D835Y),FLT3 |
A14049 | WHI-P154 | * | EGFR,Src,VEGFR | |||
A12394 | XL019 | * | **** | * | * | PDGFRβ,FLT3,c-Kit |
A14955 | S-Ruxolitinib | *** | **** | * | ** | |
A13509 | ZM 39923 HCl | * | ** | TGM2,EGFR | ||
A14012 | Decernotinib | *** | *** | **** | *** | |
A14210 | Cerdulatinib | *** | *** | *** | **** | ARK5,MST1,Fms |
A14232 | Filgotinib | *** | ** | * | * | |
A15911 | FLLL32 | * | ||||
A11241 | BMS-911543 | * | **** | ** | ** | |
A14438 | Peficitinib | |||||
A13162 | GLPG0634 analogue | |||||
A12419 | Go6976 | FLT3,PKCα,PKCβ1 | ||||
A10247 | Curcumol | |||||
A11608 | WHI-P97 | |||||
A13082 | PF-03394197 (oclacitinib) | *** | *** | ** | ** | |
A13457 | Pyridone 6 (JAK Inhibitor I) | *** | **** | **** | ||
A14132 | NSC 42834(JAK2 Inhibitor V, Z3) | |||||
A14390 | INCB39110 (Itacitinib) | |||||
A14405 | Solcitinib (GSK2586184) | |||||
A15134 | JANEX-1 | * | ||||
A15362 | Cercosporamide | *** | Mnk2, Mnk1 | |||
A15365 | TCS 21311 | * | * | *** | * | |
A15366 | ZM 449829 | **** | **** | STAT-5, EGFR, CDK4 | ||
A15389 | NSC 33994 | |||||
A16227 | ZM 39923 | **** | *** | TGM2, EGFR |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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Ruxolitinib sulfate
Catalog No. A11467 JAK1/2 inhibitorRuxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3. 了解更多 -
PF-06263276
Catalog No. A12572 pan-JAK inhibitorPF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. 了解更多 -
Tofacitinib
Catalog No. A17252 JAK3/2/1 inhibitorTofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively. 了解更多 -
JAK3 covalent inhibitor-1
Catalog No. A18926 JAK3 covalent 抑制剂JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs. 了解更多 -
TG-02 (SB1317)
Catalog No. A11962 -
BMS-986165
Catalog No. A18726 TYK2 抑制剂BMS-986165 is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. 了解更多 -
Upadacitinib (ABT-494)
Catalog No. A18316 JAK-1 抑制剂Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM. IC50 & Target: IC50: 43 nM (JAK1), 200 nM (JAK2) 了解更多 -
Abrocitinib (PF-04965842)
Catalog No. A18318 JAK1 抑制剂Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease. 了解更多 -
JAK3-IN-2
Catalog No. A18323 JAK3 抑制剂JAK3-IN-2 is a potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM. dispalys >4,300-fold selectivity over JAK1, JAK2 and TYK2, and other kinases BMX, EGFR, ITK and BTK; blocks cytokine signaling through JAK3, but not through other JAK family enzymes; inhibits IL-7 induced pSTAT5 in CD3+, CD8+ T cells with IC50 of 280 nM; sufficiently blocks the development of inflammation in a rat model of rheumatoid arthritis, while sparing hematopoiesis. 了解更多 -
PF-06700841 tosylate
Catalog No. A17176 -
Ruxolitinib Phosphate
Catalog No. A11552 JAK 抑制剂Ruxolitinib Phosphate是ruxolitinib的磷酸盐形式,ruxolitinib是一种口服生物可利用的Janus相关激酶(JAK)抑制剂,具有潜在的抗肿瘤和免疫调节活性。 了解更多 -
PF-06651600
Catalog No. A16803 JAK3 抑制剂PF-06651600是一种有效且不可逆的JAK3选择性抑制剂,IC50为33.1 nM,但对JAK1,JAK2和TYK2没有活性(IC50> 10 000 nM)。 了解更多 -
CHZ868
Catalog No. A15937 -
SB1317 (TG02)
Catalog No. A13454 CDK/JAK2/FLT3 抑制剂SB1317是细胞周期蛋白依赖性激酶(CDKs)、类FMS酪氨酸激酶-3(FLT3)和Janus激酶2(JAK2)的有效抑制剂,CDK2、JAK2和FLT3的IC50值分别为13nM、56nM和73nM。 了解更多 -
Momelotinib Mesylate
Catalog No. A21658 JAK1/JAK2 inhibitorMomelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. 了解更多 -
PF-06700841 P-Tosylate
Catalog No. A21652 dual JAK1/TYK2 inhibitorPF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. 了解更多 -
NVP-BSK805 dihydrochloride
Catalog No. A21406 JAK2 inhibitorNVP-BSK805 dihydrochloride (BSK805 dihydrochloride) is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. 了解更多 -
Oclacitinib maleate
Catalog No. A16640 JAK inhibitorOclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM). 了解更多 -
JAK/HDAC-IN-1
Catalog No. A13362 JAK2/HDAC dual inhibitorJAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. 了解更多 -
ZM39923
Catalog No. A16227 -
NS-018 maleate
Catalog No. A16226 JAK2 抑制剂NS-018 maleate是在Ba/F3-JAK2V617F细胞中具有ATP竞争性的JAK2小分子抑制剂,IC50为470nM。与其他JAK家族激酶(例如JAK1,JAK3和酪氨酸激酶2)相比,对JAK2的选择性高30-50倍。 了解更多 -
NS-018 hydrochloride
Catalog No. A16225 -
NS-018
Catalog No. A16224 -
Gusacitinib
Catalog No. A19883 SYK/JAK inhibitorGusacitinib (ASN-002) is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. 了解更多 -
PF-03394197 (oclacitinib)
Catalog No. A13082 -
XL019
Catalog No. A12394 -
Pacritinib (SB1518)
Catalog No. A12694 JAK2/FLT3 抑制剂Pacritinib (SB1518)是Janus激酶2(JAK2)和JAK2突变体JAK2V617F的口服生物利用抑制剂,无细胞试验中IC50分别为23和22 nM,具有潜在的抗肿瘤活性。Pacritinib与JAK2竞争ATP结合,这可能导致抑制JAK2活化,抑制JAK-STAT信号传导途径以及半胱天冬酶依赖性凋亡。 了解更多 -
Baricitinib (LY3009104)
Catalog No. A11329 JAK 抑制剂Baricitinib,也称为INCB028050或LY3009104,是一种选择性口服可生物利用的JAK1/JAK2抑制剂,对JAK1(5.9 nM)和JAK2(5.7 nM)具有纳摩尔浓度。 了解更多 -
NVP-BSK805
Catalog No. A11193 JAK 抑制剂NVP-BSK805是喹喔啉JAK2抑制剂对红细胞增多症的有效和选择性抑制,喹喔啉JAK2抑制剂可有效抑制小鼠和大鼠中重组人促红细胞生成素诱导的红细胞增多症和髓外红细胞生成。IC50为0.5 nM,比作用于JAK1, JAK3和TYK2选择性高20倍以上。 了解更多 -
TG-101348 (Fedratinib, SAR302503)
Catalog No. A11082 JAK2/FLT3 抑制剂TG-101348 (Fedratinib,SAR302503)是Janus相关激酶2的口服生物利用型,ATP竞争性和选择性抑制剂,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,具有潜在的抗肿瘤活性。 了解更多