JAK

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1378 Ruxolitinib (INCB018424) <1 mg/mL 61 mg/mL 61 mg/mL
S2162 AZD1480 <1 mg/mL 69 mg/mL <1 mg/mL
S2736 Fedratinib (SAR302503, TG101348) <1 mg/mL 100 mg/mL <1 mg/mL
S1134 AT9283 <1 mg/mL 76 mg/mL 38 mg/mL
S2789 Tofacitinib (CP-690550,Tasocitinib) <1 mg/mL 62 mg/mL <1 mg/mL
S8684 Selective JAK3 inhibitor 1 <1 mg/mL 70 mg/mL 9 mg/mL
S8804 PF-06700841 <1 mg/mL 78 mg/mL 78 mg/mL
S8765 PF-04965842 <1 mg/mL 65 mg/mL <1 mg/mL
S5917 Solcitinib <1 mg/mL 30 mg/mL 3 mg/mL
S5902 1,2,3,4,5,6-Hexabromocyclohexane <1 mg/mL 5 mg/mL <1 mg/mL
S5903 JANEX-1 <1 mg/mL 5 mg/mL <1 mg/mL
S5904 WHI-P97 <1 mg/mL 8 mg/mL <1 mg/mL
S2796 WP1066 <1 mg/mL 71 mg/mL <1 mg/mL
S2692 TG101209 <1 mg/mL 102 mg/mL <1 mg/mL
S2179 LY2784544 <1 mg/mL 94 mg/mL 9 mg/mL
S2686 NVP-BSK805 2HCl 3 mg/mL 113 mg/mL 15 mg/mL
S2806 CEP-33779 <1 mg/mL 36 mg/mL <1 mg/mL
S8057 Pacritinib (SB1518) <1 mg/mL 11 mg/mL <1 mg/mL
S2867 WHI-P154 <1 mg/mL 75 mg/mL <1 mg/mL
S7036 XL019 <1 mg/mL 16 mg/mL <1 mg/mL
S8004 ZM 39923 HCl <1 mg/mL 30 mg/mL 8 mg/mL
S7650 Peficitinib (ASP015K, JNJ-54781532) <1 mg/mL 65 mg/mL <1 mg/mL
S7605 Filgotinib(GLPG0634) <1 mg/mL 85 mg/mL <1 mg/mL
S7541 Decernotinib (VX-509) <1 mg/mL 78 mg/mL 20 mg/mL
S7144 BMS-911543 <1 mg/mL 36 mg/mL 22 mg/mL
S7259 FLLL32 <1 mg/mL 92 mg/mL 25 mg/mL
S2407 Curcumol <1 mg/mL 47 mg/mL 47 mg/mL
S8195 Oclacitinib maleate 18 mg/mL 90 mg/mL 90 mg/mL
S7634 Cerdulatinib (PRT062070, PRT2070) <1 mg/mL 43 mg/mL <1 mg/mL
S8541 FM-381 <1 mg/mL 20 mg/mL 2 mg/mL
S7812 Itacitinib (INCB39110) <1 mg/mL 100 mg/mL 100 mg/mL

亜型選択性的な製品

JAK製品

新JAK製品
製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1378

Ruxolitinib (INCB018424)

Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.

S2162

AZD1480

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

S2736

Fedratinib (SAR302503, TG101348)

Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.

S1134

AT9283

AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl(T315I). Phase 2.

S2789

Tofacitinib (CP-690550,Tasocitinib)

Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.

S8684

Selective JAK3 inhibitor 1

Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.

S8804

PF-06700841

PF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.

S8765

PF-04965842

PF-04965842 is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.

S5917

Solcitinib

Solcitinib is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.

S5902

1,2,3,4,5,6-Hexabromocyclohexane

1,2,3,4,5,6-Hexabromocyclohexane is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation with IC50 value to be estimated in low micromolar range.

S5903

JANEX-1

JANEX-1 is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM).

S5904

WHI-P97

WHI-P97 is a potent inhibitor of JAK-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays.

S2796

WP1066

WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. Phase 1.

S2692

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 in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.

S2179

LY2784544

Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.

S2686

NVP-BSK805 2HCl

NVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2.

S2806

CEP-33779

CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.

S8057

Pacritinib (SB1518)

Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.

S2867

WHI-P154

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.

S7036

XL019

XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1.

S8004

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.

S8538

PF-06651600

PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.

S7650

Peficitinib (ASP015K, JNJ-54781532)

Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.

S7605

Filgotinib(GLPG0634)

Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.

S7541

Decernotinib (VX-509)

Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with Ki of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.

S7144

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.

S7259

FLLL32

FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.

S2407

Curcumol

Curcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities.

S8195

Oclacitinib maleate

Oclacitinib(PF 03394197) 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. It does not inhibit a panel of 38 non-JAK kinases.

S7634

Cerdulatinib (PRT062070, PRT2070)

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.

S8541

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.

S7812

Itacitinib (INCB39110)

Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1378

Ruxolitinib (INCB018424)

Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.

S2162

AZD1480

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

S2736

Fedratinib (SAR302503, TG101348)

Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.

S1134

AT9283

AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl(T315I). Phase 2.

S2789

Tofacitinib (CP-690550,Tasocitinib)

Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.

S8684

Selective JAK3 inhibitor 1

Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.

S8804

PF-06700841

PF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.

S8765

PF-04965842

PF-04965842 is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.

S5917

Solcitinib

Solcitinib is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.

S5902

1,2,3,4,5,6-Hexabromocyclohexane

1,2,3,4,5,6-Hexabromocyclohexane is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation with IC50 value to be estimated in low micromolar range.

S5903

JANEX-1

JANEX-1 is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM).

S5904

WHI-P97

WHI-P97 is a potent inhibitor of JAK-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays.

S2796

WP1066

WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. Phase 1.

S2692

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 in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.

S2179

LY2784544

Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.

S2686

NVP-BSK805 2HCl

NVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2.

S2806

CEP-33779

CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.

S8057

Pacritinib (SB1518)

Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.

S2867

WHI-P154

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.

S7036

XL019

XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1.

S8004

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.

S8538

PF-06651600

PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.

S7650

Peficitinib (ASP015K, JNJ-54781532)

Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.

S7605

Filgotinib(GLPG0634)

Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.

S7541

Decernotinib (VX-509)

Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with Ki of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.

S7144

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.

S7259

FLLL32

FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.

S2407

Curcumol

Curcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities.

S8195

Oclacitinib maleate

Oclacitinib(PF 03394197) 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. It does not inhibit a panel of 38 non-JAK kinases.

S7634

Cerdulatinib (PRT062070, PRT2070)

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.

S8541

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.

S7812

Itacitinib (INCB39110)

Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.

Tags: JAK inhibition | JAK pathway | JAK/stat pathway | JAK drugs | JAK activation | JAK assay | JAK cancer | JAK phosphorylation | JAK2 inhibitors clinical trials | JAK inhibitors in development | JAK2 inhibitor drug | JAK inhibitor review
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