Tyk2 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S8879 Deucravacitinib (BMS-986165)

Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases.

Selective Tyk2, IC50: 0.02 nM
S7634 Cerdulatinib (PRT062070) hydrochloride

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/TYK2SykIC50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。

Selective TYK2, IC50: 0.5 nM
S0437 SAR-20347

SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively.

Selective TYK2, IC50: 0.6 nM
S7198 BIO

BIO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。

Selective TYK2, IC50: 30 nM
S0384 RO495

RO495 is a potent inhibitor of TYK2 with IC50 of 1.5nM on TYK2 as tested in cell-based pharmacological assays

Selective
S0374 GDC046

GDC046 is a potent lead analog with good kinase selectivity, physicochemical properties and pharmacokinetic profile.

Pan TYK2, Ki: 4.8 nM
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。

Pan TYK2, IC50: 1 nM-10 nM
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。

Pan TYK2, IC50: 10.76 nM
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。

Pan TYK2, Ki: 13 nM
S9676 PF-06826647

PF-06826647 (Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).

Pan TYK2, IC50: 17 nM
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。

Pan TYK2, IC50: 19 nM
S8804 PF-06700841

PF-06700841 (PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.

Pan Tyk2, IC50: 23 nM
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。

Pan TYK2, IC50: 44 nM
S8057 Pacritinib (SB1518)

Pacritinib (SB1518)是有效的选择性Janus Kinase 2 (JAK2)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。

Pan TYK2, IC50: 50 nM
S5754 Baricitinib phosphate

Baricitinib 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.

Pan TYK2, IC50: 53 nM
S2851 Baricitinib (INCB028050)

Baricitinib (LY3009104, INCB028050)是一种选择性JAK1JAK2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。

Pan TYK2, IC50: 53 nM
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。

Pan TYK2, IC50: 66 nM
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)。

Pan TYK2, IC50: 84nM
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。

Pan TYK2, IC50: 116 nM
S8765 PF-04965842

PF-04965842 is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.

Pan TYK2, IC50: 1.253 μM
S5917 Solcitinib

Solcitinib (GLPG0778, GSK2586184) is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.

Pan