JAK2 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
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。

Selective JAK2, IC50: 0.26 nM
S2214 AZ 960

AZ 960是一种新型的,ATP竞争性的JAK2抑制剂,IC50Ki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。

Selective JAK2, Ki: 0.45 nM; JAK2, IC50: <3 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。

Selective JAK2, IC50: ~0.5 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。

Selective JAK2, IC50: 1.1 nM
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。

Selective JAK2, IC50: 1.8 nM
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。

Selective JAK2, IC50: 2.2 nM
S2736 Fedratinib (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。

Selective JAK2 (V617F), IC50: 3 nM; JAK2, IC50: 3 nM
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。

Selective JAK2, IC50: 6 nM
S2796 WP1066

WP1066是一种新型JAK2STAT3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。

Selective JAK2, IC50: 2.3 μM
S7259 FLLL32

FLLL32是一种有效的 JAK2/STAT3 抑制剂,IC50 <5 μM。

Selective JAK2, IC50: <5 μM
S0391 TG-89

TG-89 is a JAK inhibitor with IC50 of 6 nM, 25 nM, 17 nM and 169 nM against JAK2, FLT3, RET and JAK3, respectively.

Selective JAK2, IC50: 11.2 μM
S1143 AG-490 (Tyrphostin B42)

AG-490 (Tyrphostin B42)是一种EGFR抑制剂,在无细胞试验中IC50为0.1 μM,作用于EGFR比作用于ErbB2选择性高135倍,对JAK2也有抑制作用,对Lck,Lyn,Btk,Syk和Src没有抑制活性。

Selective
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JAK2Flt3的强抑制剂。

Selective
S0918 Ginkgolic acid C17:1

Ginkgolic acid (C17:1) suppresses constitutive and inducible STAT3 activation through induction of PTEN and SHP-1 tyrosine phosphatase. Ginkgolic acid (C17:1) is extracted from Ginkgo biloba Leaves, Ginkgolic acid (C17:1) exhibits anticancer effects.

Selective
S6919 Brevilin A

Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.

Selective
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。

Selective
S6524 NSC 42834

NSC42834 (JAK2 Inhibitor V, Z3) is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2 with IC50 values between 10 and 30 μM.

Selective
S5588 Creatine

Creatine (Methylguanidoacetic acid) is a nitrogenous organic acid that occurs naturally in vertebrates. It facilitates the recycling of adenosine triphosphate (ATP) primarily in muscle and brain tissue.Creatine can inhibits the JAK-STAT1 signal transmission by inhibiting the interaction of IFN-γ receptors with JAK2 in an ATP-independent manner, thereby inhibiting downstream pro-inflammatory gene expression.

Selective
S3267 Kaempferol-3-O-rutinoside

Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.

Selective
S7650 Peficitinib (ASP015K)

Peficitinib (ASP015K, JNJ-54781532)是一种口服具有生物活性的 JAK 抑制剂。Phase 3。

Selective
S6899 Licochalcone D

Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.

Selective
S8152 Cucurbitacin I

Cucurbitacin-I (Elatericin B, JSI 124, NSC 521777), a natural cell-permeable triterpenoid isolated from Cucurbitaceae, is a novel selective inhibitor of JAK2/STAT3.

Selective
S2407 Curcumol

Curcumol是常见的传统中药,具有抗肿瘤活性。

Selective
S5902 1,2,3,4,5,6-Hexabromocyclohexane

1,2,3,4,5,6-Hexabromocyclohexane (NSC7908) is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation with IC50 value to be estimated in low micromolar range.

Selective
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 JAK2 (V617F), Ki: 0.245 nM; JAK2, Ki: 0.288 nM; JAK2, IC50: 3 nM
S6789 JAK Inhibitor I (Pyridone 6)

JAK Inhibitor I (Pyridone 6, CMP 6, Compound 6) is a pan-JAK inhibitor with IC50s of 1 nM, 1 nM, 5 nM and 15 nM for JAK2, TYK2, JAK3 and JAK1, respectively.

Pan JAK2, IC50: 1 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 JAK2, IC50: 1.2 nM
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。

Pan JAK2, IC50: 2.8 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 JAK2, IC50: 2.8 nM
S5243 Ruxolitinib Phosphate

Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.

Pan JAK2, IC50: 2.8 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 JAK2, IC50: 5.7 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 JAK2, IC50: 5.7 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。

Pan JAK2, IC50: 6 nM
S3566 Cerdulatinib (PRT062070)

Cerdulatinib (PRT062070, PRT2070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

Pan JAK2, IC50: 6 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 JAK2, Ki: 13 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 JAK2, IC50: 18nM
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。

Pan JAK2, IC50: 18 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 JAK2 (V617F), IC50: 19 nM; JAK2, IC50: 23 nM
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。

Pan JAK2, IC50: 20 nM
S2789 Tofacitinib (CP-690550)

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。

Pan JAK2, IC50: 20 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.

Pan JAK2, IC50: 26 nM
S0374 GDC046

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

Pan JAK2, Ki: 27.6 nM
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 JAK2, IC50: 28 nM
S9676 Ropsacitinib (PF-06826647)

Ropsacitinib (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 JAK2, IC50: 74 nM
S8804 Brepocitinib (PF-06700841)

Brepocitinib (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 JAK2, IC50: 77 nM
S8162 Upadacitinib (ABT-494)

Upadacitinib (ABT-494) is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.

Pan JAK2, IC50: 109 nM
S8684 Selective JAK3 inhibitor 1

Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.

Pan JAK2, Ki: 740 nM
S8765 Abrocitinib (PF-04965842)

Abrocitinib (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 JAK2, IC50: 803 nM
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