JAK

Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. They were initially named "just another kinase" 1 and 2 (since they were just two of many discoveries in a PCR-based screen of kinases), but were ultimately published as "Janus kinase". The name is taken from the two-faced Roman god of beginnings, endings and duality, Janus, because the JAKs possess two near-identical phosphate-transferring domains. One domain exhibits the kinase activity, while the other negatively regulates the kinase activity of the first.

Cat No.	product name
T1995	FedratinibHOT	Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
T2398	Tofacitinib CitrateHOT	Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
T1829	RuxolitinibHOT	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).
T9251	Fedratinib hydrochloride hydrate	Fedratinib hydrochloride hydrate is a potent, selective, ATP-competitive and orally active JAK2 inhibitor.
T2853	Curcumol	Curcumol, a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
T3673	Mollugin	Mollugin may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for ...
T2460	JAK 3 inhibitor IV	JAK 3 inhibitor IV is a 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 transglutam...
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 ha...
T3201	WDR5-0103	WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
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).
T6309	AZ 960	AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
T2709	TAK901	TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others....
T3069	AZD1480	AZD1480 is a novel ATP-competitive JAK2 inhibitor (IC50: 0.26 nM), selectivity act against Tyk2 and JAK3, and to a smaller extent against JAK1. AZD1480 has been ...
T3065	TG101209	TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
T6020	Pacritinib	Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
T3080	Pyridone 6	Pyridone 6(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying signi...
T6156	S-Ruxolitinib	Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
T6933	Peficitinib	Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
T2636	Decernotinib	Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
T3072	XL019	XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
T6122	CEP33779	CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
T7503	Upadacitinib	Upadacitinib (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 ...
T3998	Itacitinib	Itacitinib is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
T4210	SAR20347	SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
T4209	TAK-659 hydrochloride	TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent ...
T4227	SB1317 hydrochloride (1204918-72-8(free base))	SB1317 is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
T6321	Tofacitinib	Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
T6124	Mubritinib	Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
T5091	FM381	FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2...
T6838	FLLL32	FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).
T5049	NVP-BSK805	NVP-BSK805 is an ATP-competitive JAK2 inhibitor.
T3043	Ruxolitinib (INCB-18424) 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...
T3398	Icaritin	Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apopto...
T2485	Baricitinib	Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activiti...
T2360	Baricitinib Phosphate	Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
T2487	Cerdulatinib	Cerdulatinib is an novel oral dual Syk/JAK inhibitor.
T2653	SB1317	SB1317 is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3).
T3076	GLPG0634 analogue	GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
T1929	Filgotinib	GLPG0634(filgotinib) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.
T3620	Solcitinib	Solcitinib (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus ...
T2012	Oclacitinib	Oclacitinib(PF03394197) is a potent and selective JAKs inhibitor with IC50 of 10-99 nM; not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nM).
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....
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...
T6790	BMS911543	BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
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, ...
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).
T6104	Cerdulatinib hydrochloride	Cerdulatinib (PRT-062070) 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 S...
T3024	Avitinib	Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potent...
T6914	Oclacitinib maleate	Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which...
T6266	PP2	PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
T6916	OICR9429	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...
T3042	JAK2 Inhibitor V	NSC 42834(JAK2 Inhibitor V, Z3) is a novel specific inhibitor of Jak2, inhibiting Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner.
T2045	WHI-P131	Janex-1 is a cell-permeable, reversible, effective, ATP-competitive, and selective inhibitor of JAK3 (IC50: 78 μM); little inhibitory against JAK1/2, or Zap/Syk...
T1985	WHI-P154	WHI-P154 is a potent JAK3 inhibitor.
T4657	WHI-P97	WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxy...
T5140	WDR5-0103 hydrochloride[890190-22-4(free base)]	WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
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 ...
T5S0993	Kurarinone	Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong ...
T11711	Jaspamycin	Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity. Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to t...
T11713	JBJ-02-112-05	JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
T11714	JBJ-04-125-02	JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities. JBJ-04-125-02 is a potent, muta...
T11721L	JDTic dihydrochloride	JDTic is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
T11721	JDTic	JDTic has a very long duration of action, with effects in animals seen for up to several weeks after administration of a single dose, although its binding to the...
T8546	BD750	BD750 is an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation(IC50 of 1.5 μM and 1.1 μM i...
T16995	TAS05567	TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, ...
T17019	TCS 21311	TCS 21311 is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectivel...
T2S1040	Jolkinolide B	Jolkinolide B has potent anti-inflammatory, and antitumor activities, it is able to enhance apoptosis of human leukemic HL-60 and THP-1 cells, at least in part, ...
T2S1975	Ponicidin	Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infectio...
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...
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 infla...
T11709	JAK3 covalent inhibitor-1	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.
TN2511	1,6-O,O-Diacetylbritannilactone	1,6-O,O-Diacetylbritannilactone(OODBL) has anti-inflammatory activity, it has a potential therapeutic efficacy on inflammatory diseases especially allergic airwa...
TN2775	2-Methoxystypandrone	2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-ÎºB signaling to limit the infla...
TN3364	Agrimonolide	Agrimonolide is a potential α1 adrenergic receptor antagonist, it exerts anti-inflammatory activity, at least in part, via suppressing LPS-induced activation of...
TN3541	Broussonin E	Broussonin E could suppress inflammation by modulating macrophages activation state via inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathwa...
TMA1743	Ergosterol peroxide	Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Fox...
TN4774	Physalin A	Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate canc...
T8719	SC99	SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregatio...
T4657L	WHI-P97 HCl 211555-05-4(free base)	WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 m...
T4657L	WHI-P97 HCl 211555-05-4(free base)	WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 m...
T2341	KW2449	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-1...
T8742	JAK2 inhibitor 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 bind...
T11710	JAK-IN-5	JAK-IN-5 is an inhibitor of JAK.
T11708	JAK2-IN-4	JAK2-IN-4 is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.
T6145	ZM 39923 HCl	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...
T12266L	Ilginatinib maleate	Ilginatinib maleate is a highly active and orally bioavailable inhibitor of JAK2.
T5382	PF-06651600	PF-06651600 is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
T5492	JAK3-IN-6	JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM
TQ0010	PF-06700841	PF-06700841 is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). It also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).
TQ0037	Abrocitinib	Abrocitinib (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).
TQ0061	CHZ868	CHZ868 is a type II JAK2 inhibitor (IC50: 0.17 μM in EPOR JAK2 WT Ba/F3 cell).
TQ0196	Cucurbitacin I	Cucurbitacin I, a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
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...
TN2002	Obovatol	Obovatol has antioxidant, neuroprotective, antiinflammatory, antithrombotic and antitumour effects, it is a potent NF-κB inhibitors for Alzheimer's disease trea...
T12091L	MM-589 TFA	MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
T12091	MM-589	MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
T12266L2	Ilginatinib hydrochloride	Ilginatinib hydrochloride is a highly active and orally bioavailable inhibitor of JAK2.
T12266	Ilginatinib	Ilginatinib is a highly active and orally bioavailable inhibitor of JAK2.
T11690	ITK inhibitor 2	ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor , with an IC50 of 2 nM.
T12427	PF-06700841 (P-Tosylate)	PF-06700841 P-Tosylate is a potent dual inhibitor of Janus kinase 1 (JAK1) and TYK2 (IC50s of 17 nM and 23 nM, respectively).
T12549	JAK-IN-11	JAK-IN-11 is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.
T14331	Gusacitinib	Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
T14687	BMS-986165	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 ...
T10424	AZ-3	AZ-3 is a potent and selective JAK1 inhibitor (IC50: 34 nM).
T10431	AZD4205	AZD4205 is a selective JAK1 inhibitor (IC50: 73 nM) and weakly inhibits JAK2/JAK3 (IC50: >14.7, >30 μM).
T15037	Momelotinib Mesylate	Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
T15038	Momelotinib sulfate	Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
T15096	Delgocitinib	Delgocitinib is a novel and specific inhibitor of JAK (IC50s: 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2).
T15605	JAK/HDAC-IN-1	JAK/HDAC-IN-1 is an effective JAK2/HDAC dual inhibitor (IC50s: 4 and 2 nM for JAK2 and HDAC). It also shows antiproliferative and proapoptotic activities in seve...
T15606	JAK1-IN-4	JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in ...
T10009	JAK3-IN-7	JAK3-IN-7 is an effective and selective JAK3 inhibitor (IC50 <0.01 μM) extracted from patent WO2011013785A1.
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 ...