DC Chemicals · Research reagents

JAK

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AZD1480 chemical structureDC5032

AZD1480

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. IC50 value: 0.26 nM Target: JAK2 in vitro: AZD1480 demonstrated…

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BMS-911543 chemical structureDC4175

BMS-911543

BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively).

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JAK2 Inhibitor V,Z3 chemical structureDC7436

JAK2 Inhibitor V,Z3

JAK2 Inhibitor V, Z3 is a cell-permeable pyridinylbutanone compound that inhibits both JAK2 and the active V167F mutant cellular autophosphorylation. JAK2 Inhibitor V, Z3 displays no effect against cellular Tyk 2…

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TG101209 chemical structureDC7317

TG101209

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, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.

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XL019 chemical structureDC5022

XL019

XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1; shows good biochemical and cellular potency against JAK2 with good selectivity against the Janus Kinase family as well…

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S-Ruxolitinib (INCB018424) chemical structureDC5199

S-Ruxolitinib (INCB018424)

INCB018424 potently and selectively inhibits JAK2V617F-mediated signaling and proliferation in Ba/F3 cells and HEL cells. INCB018424 markedly increases apoptosis in a dose dependent manner in Ba/F3 cells. INCB018424…

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Solcitinib（GLPG0778） chemical structureDC8169

Solcitinib（GLPG0778）

Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of…

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WHI-P258 chemical structureDC8080

WHI-P258

WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated Ki of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM[1][2].

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Upadacitinib chemical structureDC10431

Upadacitinib

Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.

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FM-381 chemical structureDC10826

FM-381

FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively.

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Itacitinib(INCB039110) chemical structureDC12378

Itacitinib(INCB039110)

Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.

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JAK2 inhibitor G5-7 chemical structureDC11136

JAK2 inhibitor G5-7

JAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor that selectively inhibits JAK2-mediated phosphorylation and activation of EGFR and STAT3 by binding to JAK2; demonstrates inhibitor of U87MG/EGFR and…

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AZ-960 chemical structureDC7367

AZ-960

AZ960 also inhibits many kinases less than 50% at a concentration of 0.1 μM such as JAK3 (IC50=9 nM), TrkA, Aurora, and ARK5. In cells, AZ 960 inhibits the phosphorylation of STAT5 in TEL-JAK2 cells with an average…

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Gandotinib(LY2784544) chemical structureDC7665

Gandotinib(LY2784544)

Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.

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