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Home >> Signaling Pathways >> Chromatin/Epigenetics >> Pim

Pim(Pim激酶)

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.

  1. Cat.No. 产品名称 Information
  2. GC34964 (1S,3R,5R)-PIM447 dihydrochloride (1S,3R,5R)-PIM447 (dihydrochloride)是PIM的抑制剂，来自专利US 20100056576 A1化合物实例72。对Pim1，Pim2和Pim3的IC50分别为0.095，0.522和0.369 μM。
  3. GC12660 AZD1208 A pan-Pim kinase inhibitor
  4. GC35447 AZD1208 hydrochloride A pan-Pim kinase inhibitor
  5. GC39485 CK2/ERK8-IN-1 A dual inhibitor of CK2 and ERK8
  6. GC13056 CX-6258 A pan-Pim kinase inhibitor
  7. GC19747 CX-6258 HCl A pan-Pim kinase inhibitor
  8. GC35762 CX-6258 hydrochloride hydrate A pan-Pim kinase inhibitor
  9. GC32958 GDC-0339 GDC-0339是Pim激酶抑制剂,作用于BaF3PIM1时,IC50为43.6nM。
  10. GC33253 GNE-955 GNE-955是有效的泛Pim激酶抑制剂，Ki分别为18，110，8nM。
  11. GC12359 Hispidulin A flavonoid with diverse biological activities
  12. GC13154 LKB1(AAK1 dual inhibitor) LKB1(AAK1 dual inhibitor) 是一种有效的多激酶抑制剂，对 Pim1/AKK1/MST2/LKB1 的 Kd 值分别为 35 nM/53 nM/75 nM/380 nM，并且还抑制 MPSK1 和 TNIK。
  13. GC34138 M-110 M-110是Pim激酶抑制剂，抑制前列腺癌细胞系增殖IC50为0.6-0.9uM。
  14. GC49412 NSC 756093 An inhibitor of the GBP1-Pim-1 protein-protein interaction
  15. GC19419 PIM inhibitor 1 phosphate Uzansertib (INCB053914) phosphate 是一种具有口服活性的 ATP 竞争性泛 PIM 激酶抑制剂，对 PIM1、PIM2、PIM3 的 IC50 分别为 0.24 nM、30 nM、0.12 nM。 PIM inhibitor 1 phosphate 对多种血液肿瘤细胞系具有广泛的抗增殖活性。
  16. GC13558 PIM-1 Inhibitor 2 A potent PIM-1 kinase inhibitor
  17. GC36918 PIM-447 dihydrochloride PIM447是泛PIM激酶抑制剂，对PIM1，PIM2，PIM3的 Ki 分别为6，18，9 nM。
  18. GC65278 PIM1-IN-1 PIM1-IN-1 是一种有效、高度选择性的 PIM1/3 抑制剂，对 PIM1，PIM2 和 PIM3 的 IC50 值分别为 7，5530 和 70 nM。PIM1-IN-1 抑制 PIM 下游蛋白 BAD 的磷酸化，EC50 值为 262 nM，而对 FLT3 或 hERG 无作用。具有抗增殖、抗肿瘤作用。
  19. GC19398 PIM447 PIM447 (LGH447) 是一种有效的、口服的、选择性的泛 PIM 激酶抑制剂，对 PIM1、PIM2 和 PIM3 的 Ki 值分别为 6、18 和 9 pM。 PIM447 具有双重抗骨髓瘤和骨保护作用。 PIM447 诱导细胞凋亡。
  20. GC65201 Quercetagetin A selective Pim-1 inhibitor
  21. GC13488 R8-T198wt R8-T198wt 是一种细胞可渗透的羧基末端 p27Kip1 肽，通过抑制 Pim-1 激酶表现出抗肿瘤活性。
  22. GC64774 SEL24-B489 SEL24-B489 是有效的、I 型的、口服有效的、PIM 和 FLT3-ITD 的双抑制剂，其对PIM1、PIM2 和 PIM3 的 Kd 值分别为 2 nM、2 nM、和 3 nM。
  23. GC16497 SGI-1776 free base A potent inhibitor of Pim kinases
  24. GC37651 SMI-16a A Pim-1 kinase inhibitor
  25. GC11104 SMI-4a A Pim kinase inhibitor
  26. GC17178 TCS PIM-1 1 A Pim-1 kinase inhibitor
  27. GC11990 TCS-PIM-1-4a TCS-PIM-1-4a (SMI-4a) 是一种泛 Pim 激酶抑制剂，通过激活 AMPK 来阻断 mTORC1 的活性。 TCS-PIM-1-4a 可杀死多种髓系和淋巴系细胞系（IC50 值范围为 0.8 μM 至 40 μM）。
  28. GC19361 TP-3654 A Pim kinase inhibitor

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