Pim

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
S2198 SGI-1776 free base <1 mg/mL 81 mg/mL 81 mg/mL
S8005 SMI-4a <1 mg/mL 55 mg/mL 32 mg/mL
S6497 SMI-16a <1 mg/mL 53 mg/mL 4 mg/mL
S1050 TCS PIM-1 1 ˂1 mg/mL 73 mg/mL ˂1 mg/mL
S8800 INCB053914 -1 mg/mL 50 mg/mL -1 mg/mL
S6774 TP-3654 <1 mg/mL 84 mg/mL 6 mg/mL
S7985 PIM447 (LGH447) <1 mg/mL 88 mg/mL '88 mg/mL
S7104 AZD1208 <1 mg/mL 75 mg/mL ''<1 mg/mL
S7041 CX-6258 89 mg/mL 57 mg/mL 1 mg/mL

亜型選択性的な製品

Pim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
S2198

SGI-1776 free base

SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. Phase 1.

S8005

SMI-4a

SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.

S6497

SMI-16a

SMI-16a is a selective Pim kinase inhibitor with IC50 values of 150 nM and 20 nM for Pim1 and Pim2 respectively.

S1050

TCS PIM-1 1

TCS PIM-1 1 is a potent and selective inhibitor of ATP-competitive Pim-1 kianse with IC50 of 50 nM, shows good selectivity over Pim-2 and MEK1/MEK2 with IC50 > 20000 nM.

S8800

INCB053914

INCB053914 is a novel, ATP-competitive, small molecule, pan-inhibitor of PIM kinases with IC50 values of 0.24 nM, 30 nM and 0.12 nM for PIM1, PIM2 and PIM3 respectively in biochemical assays.

S6774

TP-3654

TP-3654 is the second-generation PIM inhibitor with Ki values of 5 nM, 239 nM, and 42 nM for PIM-1, PIM-2 and PIM-3, respectively.

S7985

PIM447 (LGH447)

PIM447 is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis.

S7104

AZD1208

AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.

S7041

CX-6258

CX-6258 HCl is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.

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
S2198

SGI-1776 free base

SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. Phase 1.

S8005

SMI-4a

SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.

S6497

SMI-16a

SMI-16a is a selective Pim kinase inhibitor with IC50 values of 150 nM and 20 nM for Pim1 and Pim2 respectively.

S1050

TCS PIM-1 1

TCS PIM-1 1 is a potent and selective inhibitor of ATP-competitive Pim-1 kianse with IC50 of 50 nM, shows good selectivity over Pim-2 and MEK1/MEK2 with IC50 > 20000 nM.

S8800

INCB053914

INCB053914 is a novel, ATP-competitive, small molecule, pan-inhibitor of PIM kinases with IC50 values of 0.24 nM, 30 nM and 0.12 nM for PIM1, PIM2 and PIM3 respectively in biochemical assays.

S6774

TP-3654

TP-3654 is the second-generation PIM inhibitor with Ki values of 5 nM, 239 nM, and 42 nM for PIM-1, PIM-2 and PIM-3, respectively.

S7985

PIM447 (LGH447)

PIM447 is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis.

S7104

AZD1208

AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.

S7041

CX-6258

CX-6258 HCl is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.