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.
Products for Pim
- Cat.No. Product Name Information
- GC34964 (1S,3R,5R)-PIM447 dihydrochloride (1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.
- GC35447 AZD1208 hydrochloride AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor.
- GC35762 CX-6258 hydrochloride hydrate CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
- GC32958 GDC-0339 GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma.
- GC33253 GNE-955 GNE-955 is a potent and orally active pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.
- GC12359 Hispidulin Partial positive allosteric modulator at the benzodiazepine receptor
- GC34138 M-110 M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
- GC19419 PIM inhibitor 1 phosphate Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. PIM inhibitor 1 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
- GC36918 PIM-447 dihydrochloride A pan-Pim kinase inhibitor
- GC65278 PIM1-IN-1 PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.
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GC19398
PIM447
PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.
- GC65201 Quercetagetin Quercetagetin (6-Hydroxyquercetin) is a flavonoid.
- GC64774 SEL24-B489 SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively.
- GC37651 SMI-16a A Pim-1 kinase inhibitor
- GC11990 TCS-PIM-1-4a Pim inhibitor
- GC19361 TP-3654 TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.