Pim

シグナル伝達経路

研究分野

  • 阻害剤の選択性比較
  • 溶解度
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
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

製品コード 製品説明 文献中の使用例 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.

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).

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. 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.