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Pim

Pim protein kinases are a family of serine/threonine kinases consisting of three members of Ca2+/calmodulin-dependent protein kinases, including PIM1, PIM2 and PIM3, that are responsible for cell cycle regulation and antiapoptotic activity as well as homing and migration of receptor tyrosine kinases mediated through the JAK/STAT pathway. All three pim protein kinases share high homology at the amino acid level and hence exhibit greatly overlapping functions, in which 71% and 61% identical amino acids have been found between PIM1/PIM3 and between PIM1/PIM2 respectively. PIM1 comprises two isoforms of 34 and 44 kDa respectively; while PIM2 comprises three isoforms of 34, 37 and 40 kDa respectively. However, PIM3 comprises only one protein.

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  1. Cat.No. Product Name Information
  2. A3556 LKB1 (AAK1 dual inhibitor)

    LKB1 is a selective inhibitor of Pim-1 kinase with Kd value of 35 nM [1].

  3. A3338 CX-6258 hydrochloride hydrate CX-6258 is a potent, orally efficacious pan-Pim kinases Inhibitor with excellent biochemical potency and kinase selectivity. in vitro: CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). At 0.5 uM of CX-6258, only Pim-1, Pim-2, Pim-3, and Flt-3 of the 107 kinases tested were inhibited by more than 80%, showing excellent selectivity. CX-6258 was also shown to be a reversible inhibitor of Pim-1 (Ki=0.005 uM).
  4. A3337 CX-6258 CX-6258 is a potent, orally efficacious pan-Pim kinases Inhibitor with excellent biochemical potency and kinase selectivity. in vitro: CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). At 0.5 uM of CX-6258, only Pim-1, Pim-2, Pim-3, and Flt-3 of the 107 kinases tested were inhibited by more than 80%, showing excellent selectivity. CX-6258 was also shown to be a reversible inhibitor of Pim-1 (Ki=0.005 uM).
  5. A4193 SMI-4a SMI-4a is a selective inhibitor of Pim1 with IC50 value of 17 nM [1] [2].
  6. A4192 SGI-1776 free base

    SGI-1776 free base, N-((1-methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine, is a potent ATP-competitive inhibitor of the serine/threonine family of Pim kinase, an enzyme regulating cell survival.

  7. A3962 AZD1208 AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases and is currently undergoing Phase I testing and dose escalation studies in AML.
  8. A4519 PIM-1 Inhibitor 2 Potent Pim-1 kinase inhibitor (Ki = 91 nM).
  9. A4520 R8-T198wt Cell-permeable peptide inhibitor of Pim-1 kinase, derived from p27Kip1. Inhibits Pim-1 phosphorylation of p27Kip1 and Bad; induces cell cycle arrest (at G1) and apoptosis in DU145 prostate cancer cells. Also inhibits Pim-1-dependent growth of DU145 cells in vitro and in vivo. Displays no effect on the growth of normal prostate epithelial RPWE-1 cells at concentrations of 10 and 20 μM.
  10. A4521 TCS PIM-1 1 ATP-competitive Pim-1 kinase inhibitor that displays selectivity over Pim-2 and MEK1/2 (IC50 values are 50, > 20000 and > 20000 nM for Pim-1, Pim-2 and MEK1/2 respectively).

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