JAK

The JAK-STAT signalling pathway is a chain of interactions between proteins in a cell, and is involved in processes such as immunity, cell division, cell death and tumour formation. There are 4 JAK proteins: JAK1, JAK2, JAK3 and TYK2. JAKs contains a FERM domain (approximately 400 residues), an SH2-related domain (approximately 100 residues), a kinase domain (approximately 250 residues) and a pseudokinase domain (approximately 300 residues). The kinase domain is vital for JAK activity, since it allows JAKs to phosphorylate (add phosphate groups to) proteins.

Cat No.	product name
T2341	KW-2449	KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R...
T6515	Go6976	Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and ...
T9251	Fedratinib hydrochloride hydrate	Fedratinib hydrochloride hydrate is a potent, selective, ATP-competitive and orally active JAK2 inhibitor.
T1829	Ruxolitinib	Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC50: 3.3/2.8 nM) and is relatively less selective for JAK3 (IC50: 322 nM).
T38624	Fosifidancitinib	Fosifidancitinib is a potent inhibitor of JAK 1 and JAK 3.
T2709	TAK-901	TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others....
T3201	WDR5-0103	WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
T6S1966	Curculigoside	1. Curculigoside can prevent bone loss , improve osteogenesis and inhibit osteoclastogenesis of hAFSCs, suggesting its potential use to regulate hAFSC osteogenic...
T6309	AZ960	AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
T6838	FLLL32	FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).
TN1059	Ganoderic acid B	Ganoderic acid B is a chemical marker in quality control of G. lucidum and related products. Ganoderic acid B-containing herbs has potential influence towards th...
T2035	WHI-P258	WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of new...
T3065	TG101209	TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
T2360	Baricitinib phosphate	Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
T2398	Tofacitinib Citrate	Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
T2853	Curcumol	Curcumol, a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
T6321	Tofacitinib	Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
T2638	Gandotinib	LY2784544(Gandotinib) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3....
T2156	WP1066	WP1066 is a inhibitor of JAK2 (IC50: 2.30 μM) and STAT3 (IC50: 2.43 μM) in HEL cells; shows activity to JAK2, STAT3/5, and ERK1/2, not JAK1 and JAK3. WP1066 has ...
T6217	LFM-A13	LFM-A13（IC50=2.5 μM）, a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and...
T1849	Momelotinib	Momelotinib is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with ...
T3068	AT9283	AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
T2S1975	Ponicidin	Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infectio...
TJS1779	Protosappanin A	Protosappanin A has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IÎºB/NF-ÎºB inflammat...
T8719	SC99	SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation...
T3398	Icaritin	Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apopto...
T6916	OICR-9429	OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemi...
T2600	AG490	AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, L...
T9195	SHR0302	SHR0302 is a JAK inhibitor that binds JAK1 with stronger affinity than others (Selectivity for JAK1 is more than 10 times for JAK2, 77 times for JAK3, 420 times ...
T14331	Gusacitinib	Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
T5S0167	Atractylenolide I	1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reductio...
T21503	(E/Z)-Zotiraciclib	(E/Z)-Zotiraciclib inhibits CDK2, JAK2, and FLT3 effectively with IC50s of 13, 73, and 56 nM, respectively.
T1985	WHI-P154	WHI-P154 is a potent JAK3 inhibitor.
T8742	G5-7	JAK2 inhibitor G5-7 is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding ...
T2378	RGB-286638 free base	RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3...
T1995	Fedratinib	Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
T6920	ON123300	ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).
T14687	Deucravacitinib	BMS-986165 inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of ...
T22338	2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide	GDC046, a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.
T2485	Baricitinib	Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activiti...
T6145	ZM39923 hydrochloride	ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase...
T3043	Ruxolitinib phosphate	Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivit...
T9826	GDC-0214	GDC-0214 is an inhaled small-molecule JAK1 inhibitor and reduces fractional exhaled nitric oxide (Feno).
T3072	XL019	XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
T7123	AMG-47a	AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the lev...
T22319	DTP3	DTP3 is a selective MKK7/GADD45β inhibitor, which inhibits cancer-selective NF-κB survival pathway.
T4672	Brevilin A	Brevilin A is a sesquiterpene lactone isolated from Centipeda minima, inhibits janus kinase activity and blocks STAT3 signaling in cancer cells with anti-tumor a...
T4S1499	Ginsenoside Rk1	Ginsenoside Rk1 is a component created by processing the ginseng plant at high temperatures. Ginsenoside Rk1 has an anti-inflammatory effect, suppresses the acti...
T35341	NVP-BSK805 dihydrochloride	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。
T22142	RO8191	RO8191 (CDM-3008), an imidazonaphthyridine compound, is an agonist of interferon (IFN) receptor.