JAK/STAT Signaling

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Cat. No.	Product Name	Field of Application
DC10105	SH5-07 Featured	SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9±0.6 μM in in vitro assay.
DC10514	SMI-16a Featured	SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively.
DC7503	SMI 4a Featured	SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modest potent to Pim-2, does not significantly inhibit other serine/threonine- or tyrosine-kinases.
DC8169	Solcitinib（GLPG0778） Featured	Solcitinib, also known as GSK2586184 or GLPG0778, is a Janus kinase 1 (JAK1) inhibitor.
DC10139	Stat5 Inhibitor(STAT5-IN-1) Featured	Stat5 Inhibitor is a cell permeable nonpetidic nicotinoyl hydrazone which suppresses Stat5 via binding to the SH2 domain.
DC7514	TCS PIM-1 1 Featured	TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).
DC7317	TG101209 Featured	TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations; TG101209 inhibit BRD4 activity with IC50 of 130 nM.
DC7318	TG101348(Fedratinib) Featured	TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3, TG-101348 also inhibit BRD4 with IC50 of 340 nM.
DC8511	TG-46 Featured	TG-46 is an inhibitor of JAK2, FLT3, RET, JAK3 with IC50 values of 6nM, 25nM, 17nM, 169nM respectively.
DC8510	TG-89 Featured	TG-89 is a JAK inhibitor. It has IC50 values of 6, 25, 17 and 169 nM against JAK2, FLT3, RET and JAK3 respectively.
DC8736	Tofacitinib Featured	Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.
DC5165	Tofacitinib (CP-690550) Citrate Featured	Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.
DC10031	TP-3654 Featured	TP-3654 is a small molecule pan-Pim (PIM) kinase inhibitor.
DC10431	Upadacitinib Featured	Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM.
DC7581	WHI-P154 Featured	WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.
DC8080	WHI-P258 Featured	WHI-P258 is a negative control for JAK3 inhibitors.
DC9494	WHI-P97 Featured	WHI-P97 is a rationally designed potent inhibitor of JAK-3.
DC5022	XL019 Featured	XL019 is an orally bioavailable inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity.
DC11436	YLT-11 Featured	YLT-11 is a novel and specific PLK4 inhibitor with IC50 of 22 nM and Kd of 5.2 nM.
DC7436	JAK2 Inhibitor V,Z3 Featured	Z3(NSC 42834), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
DC7667	ZM 39923 hydrochloride Featured	ZM 39923 is an inhibitor of JAK3 (IC50 = 79 nM) that less potently inhibits epidermal growth factor receptor, JAK1, and cyclin-dependent kinase 4 (IC50s = 2.4, 40, and 10 µM, respectively).
DC5199	S-Ruxolitinib (INCB018424) Featured	S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3.
DC40051	Fedratinib hydrochloride hydrate	Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
DC40121	(R)-Lisofylline	(R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 μM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research.
DC40139	JAK-IN-5 hydrochloride	JAK-IN-5 hydrochloride is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
DC40168	SHR0302	SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects.
DC40459	FM-479 Featured	FM-479 is the negative control of FM-381 and has no activity on JAK3 or other kinases.
DC40513	BD750 Featured	BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
DC40757	ZM 449829	ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3.
DC41052	JAK2-IN-6	JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.

JAK/STAT Signaling

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