DC8309 |
Ruxolitinib Phosphate
Featured
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Ruxolitinib Phosphate is a potent and selective Janus kinase (JAK1, IC50 = 5.9 nM and JAK2, IC50 = 5.7 nM) inhibitor. |
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DC10823 |
SAR-20347
Featured
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SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively. |
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DC8169 |
Solcitinib(GLPG0778)
Featured
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Solcitinib, also known as GSK2586184 or GLPG0778, is a Janus kinase 1 (JAK1) inhibitor. |
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DC7317 |
TG101209
Featured
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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. |
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DC7318 |
TG101348(Fedratinib)
Featured
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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. |
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DC8511 |
TG-46
Featured
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TG-46 is an inhibitor of JAK2, FLT3, RET, JAK3 with IC50 values of 6nM, 25nM, 17nM, 169nM respectively. |
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DC8510 |
TG-89
Featured
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TG-89 is a JAK inhibitor. It has IC50 values of 6, 25, 17 and 169 nM against JAK2, FLT3, RET and JAK3 respectively. |
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DC8736 |
Tofacitinib
Featured
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Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3. |
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DC5165 |
Tofacitinib (CP-690550) Citrate
Featured
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Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3. |
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DC10431 |
Upadacitinib
Featured
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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. |
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DC7581 |
WHI-P154
Featured
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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. |
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DC8080 |
WHI-P258
Featured
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WHI-P258 is a negative control for JAK3 inhibitors. |
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DC9494 |
WHI-P97
Featured
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WHI-P97 is a rationally designed potent inhibitor of JAK-3.
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DC5022 |
XL019
Featured
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XL019 is an orally bioavailable inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity. |
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DC7436 |
JAK2 Inhibitor V,Z3
Featured
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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. |
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DC7667 |
ZM 39923 hydrochloride
Featured
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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). |
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DC5199 |
S-Ruxolitinib (INCB018424)
Featured
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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. |
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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. |
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DC40139 |
JAK-IN-5 hydrochloride |
JAK-IN-5 hydrochloride is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283. |
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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. |
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DC40459 |
FM-479
Featured
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FM-479 is the negative control of FM-381 and has no activity on JAK3 or other kinases.
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DC40513 |
BD750
Featured
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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. |
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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. |
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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. |
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DC41406 |
Coumermycin A1 |
Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria. |
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DC42324 |
JAK2-IN-7 |
JAK2-IN-7 is a selective JAK2 with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities. |
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DC42325 |
(3S,4S)-Tofacitinib |
(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM. |
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DC44160 |
JAK2/FLT3-IN-1 |
JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity. |
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DC46855 |
Deuruxolitinib |
Deuruxolitinib (CTP-543), a deuterated Ruxolitinib, modulates the activity of JAK1/JAK2. Deuruxolitinib can be used for the research hair loss disorders (from patent WO2017192905A1, compound I). |
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DC46856 |
JAK2/FLT3-IN-1 TFA |
JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity. |
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