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JAK
T1829 Ruxolitinib Ruxolitinib is an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.
T1849 CYT387 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 JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induc
T1929 Filgotinib (GLPG0634) 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.
T1985 WHI-P154 WHI-P154 is a potent JAK3 inhibitor.
T1995 Fedratinib (SAR302503, TG101348) Fedratinib is an orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity.
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).
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 therapeutics.
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 or SRC tyrosine kinases.
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 been used in trials studying the treatment of Melanoma, Brain Cancer, Solid Tumors, and Central Nervous System Neoplasms.
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, EGFR.
T2360 Baricitinib phosphate Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
T2398 Tofacitinib citrate Tofacitinib citrate (CP-690550 citrate) is a novel JAK3 inhibitor (IC50: 1 nM), 20- to 100-fold less potent against JAK2/1.
T2460 ZM 39923 hydrochloride ZM 39923 hydrochloride 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 transglutaminase.
T2485 Baricitinib Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
T2487 Cerdulatinib Cerdulatinib is an novel oral dual Syk/JAK inhibitor.
T2600 AG-490 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, Lck, Syk, Btk, and Src.
T2636 Decernotinib(VX-509) 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.
T2638 Gandotinib (LY2784544) 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.
T2653 SB1317 SB1317 is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3)。
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.
T2853 Curcumol Curcumol, a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
T3042 NSC 42834 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.
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 selectivity for JAK1/2 versus JAK3.
T3065 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 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).
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 used in trials studying the treatment of Solid Malignancies, Post-Polycythaemia Vera, Primary Myelofibrosis (PMF), and Essential Thrombocyt
T3072 XL019 XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
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.
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 significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.
T3201 WDR5-0103 WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
T3398 Icaritin Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6/JAK2/STAT3 signaling.
T3620 Solcitinib Solcitinib (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus erythematosus.
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 a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a
T3998 Itacitinib Itacitinib is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
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 toward both SYK and FLT3.
T4210 SAR-20347 SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
T4227 SB1317(TG-02) hydrochloride (937270-47-8(free base)) SB1317 is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
T6020 Pacritinib (SB1518) Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
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 Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
T6124 Mubritinib (TAK 165) Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
T6156 S-Ruxolitinib (INCB018424) Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
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.
T6294 NVP-BSK805 2HCl (1092499-93-8(free base)) NVP-BSK805 2HCl(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.
T6309 AZ 960 AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
T6321 Tofacitinib Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
T6790 BMS-911543 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.
T6838 FLLL32 FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).
T6914 Oclacitinib maleate <p>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 did not inhibit a panel of 38 non-JAK kinases.</p>
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 leukemia cells in vitro.
T6933 Peficitinib (ASP015K, JNJ-54781532) Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
T6122 CEP-33779 CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
T7503 Upadacitinib (ABT-494) 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 nM.
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