JAK

Inhibitory Selectivity

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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Decernotinib

Catalog No. A14012
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JAK3 抑制剂

Decernotinib是Vertex开发的口服选择性Janus激酶3（JAK3）抑制剂。了解更多

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ZM39923

Catalog No. A16227
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JAK1/3 抑制剂

ZM39923是一种JAK1/3抑制剂，pIC50为4.4/7.1，对JAK2几乎没有活性，对EGFR的作用中等。还发现对转谷氨酰胺酶敏感。了解更多

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INCB018424 (Ruxolitinib)

Catalog No. A11041
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JAK1/2 抑制剂

INCB018424 (Ruxolitinib)是有效和选择性的Janus相关激酶JAK1/2抑制剂，对JAK1，JAK2和JAK3的IC50分别为2.7、4.5和332 nM。了解更多

Product Citations (6)

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Rasmus Siersbek, .et al. IL6/STAT3 Signaling Hijacks Estrogen Receptor α Enhancers to Drive Breast Cancer Metastasis, Cancer cell, 2020, Jul 6;S1535-6108(20)30311-1 PMID: 32679107
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Kagoya Y, .et al. JAK2V617F+ myeloproliferative neoplasm clones evoke paracrine DNA damage to adjacent normal cells through secretion of lipocalin-2., Blood., 2014, Nov 6;124(19):2996-3006 PMID: 25217696
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GLPG0634

Catalog No. A13162
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JAK1 抑制剂

GLPG0634是一种口服的JAK1(Janus激酶1)选择性抑制剂，对 JAK1/JAK2/JAK3的IC50值为50-200 nM。用于治疗类风湿性关节炎和潜在的其他炎性疾病。了解更多

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- Keisuke Nishimura, .et al. Tofacitinib facilitates the expansion of myeloid-derived suppressor cells and ameliorates arthritis in SKG mice., Arthritis Rheumatol., 2015, Apr;67(4):893-902 PMID: 25545152
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INCB39110 (Itacitinib)

Catalog No. A14390
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JAK1 抑制剂

INCB39110 (Itacitinib)是一种有效的JAK1酪氨酸激酶抑制剂，目前正在II期试验中，用于治疗类风湿关节炎，骨髓纤维化，类风湿关节炎和斑块状牛皮癣。了解更多

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- Czech J, .et al. JAK2V617F but not CALR mutations confer increased molecular responses to interferon-α via JAK1/STAT1 activation, Leukemia, 2018, Nov 23 PMID: 30470838
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CYT387 sulfate salt

Catalog No. A15056
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JAK 抑制剂

CYT387 sulfate salt是JAK1/JAK2的ATP竞争性抑制剂，IC50为11 nM/18 nM，是JAK3的约10倍选择性。了解更多

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Baricitinib (LY3009104)

Catalog No. A11329
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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

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- Yuki Sasaki, .et al. Blockade of the CXCR3/CXCL10 axis ameliorates inflammation caused by immunoproteasome dysfunction, JCI Insight, 2022, Apr 8;7(7) PMID: 35393946
- Yutian Lei, .et al. A multicenter blinded preclinical randomized controlled trial on Jak1/2 inhibition in MRL/MpJ-Fas lpr mice with proliferative lupus nephritis predicts low effect size, Kidney Int, 2021, Feb 16 PMID: 33607177
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Cerdulatinib

Catalog No. A14210
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multi-targeted tyrosine kinase 抑制剂

Cerdulatinib (PRT-062070)是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。了解更多

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ZM 39923 HCl

Catalog No. A13509
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JAK3 抑制剂

ZM 39923 HCl是JAK3抑制剂（IC50 = 79 nM），其抑制表皮生长因子受体，JAK1和细胞周期蛋白依赖性激酶4（IC50s分别为2.4、40和10 M）的抑制作用较小。了解更多

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Cyt387 (Momelotinib)

Catalog No. A10263
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JAK 抑制剂

Cyt387 (Momelotinib)是Janus激酶JAK1和JAK2的抑制剂，可作为ATP竞争者，IC50值分别为11和18 nM。了解更多

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- Alex Bainbridge, .et al. IKBKE activity enhances AR levels in advanced prostate cancer via modulation of the Hippo pathway, Nucleic Acids Research, 2020, April
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Pyridone 6 (JAK Inhibitor I)

Catalog No. A13457
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JAK 抑制剂

JAK Inhibitor I 是JAK1、JAK2和JAK3的一种高效、可逆、细胞通透性和ATP竞争性抑制剂。了解更多

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Solcitinib (GSK2586184)

Catalog No. A14405
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JAK1 抑制剂

Solcitinib (GSK2586184)是Janus激酶1（JAK1）抑制剂。了解更多

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Baricitinib phosphate

Catalog No. A15014
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JAK 抑制剂

Baricitinib phosphate是一种选择性的JAK1和JAK2抑制剂，IC50为5.9 nM和5.7 nM，选择性是JAK3和Tyk2的?70和?10倍，对c-Met和Chk2没有抑制作用。了解更多

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PF-03394197 (oclacitinib)

Catalog No. A13082
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JAK1 抑制剂

PF-03394197 (oclacitinib)是有效的JAK1抑制剂。了解更多

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- Banovic F, .et al. Immunomodulatory in vitro effects of oclacitinib on canine T-cell proliferation and cytokine production, Vet Dermatol, 2018, Nov 12 PMID: 30417482
- Nicholas B, .et al. Susceptibility to influenza virus infection of bronchial biopsies in asthma, J Allergy Clin Immunol, 2017, Jul;140(1):309-312.e4 PMID: 28259448
- Fukuyama T, .et al. Topically Administered Janus-Kinase Inhibitors Tofacitinib and Oclacitinib Display Impressive Antipruritic and Anti-Inflammatory Responses in a Model of Allergic Dermatitis., J Pharmacol Exp Ther., 2015, Sep;354(3):394-405 PMID: 26159873
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Filgotinib

Catalog No. A14232
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JAK 抑制剂

Filgotinib是一种选择性的JAK1抑制剂，对于JAK1，JAK2，JAK3和TYK2的IC50分别为10 nM，28 nM，810 nM和116 nM。了解更多

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S-Ruxolitinib

Catalog No. A14955
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JAK 抑制剂

S-Ruxolitinib是INCB018424的手性化合物，是一种有效且选择性的小分子Janus激酶1（JAK1）和JAK2抑制剂。了解更多

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NVP-BSK805

Catalog No. A11193
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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

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PRT 062070 (Cerdulatinib)

Catalog No. A14147
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Dual Syk and JAK 抑制剂

PRT 062070 (Cerdulatinib)是一种新型的口服双脾酪氨酸激酶（Syk）和janus激酶（JAK）抑制剂。Cerdulatinib优先抑制各种细胞类型中JAK1和JAK3依赖性细胞因子介导的信号传导和功能性反应。了解更多

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