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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SMI-4a是ATP竞争性Pim激酶抑制剂，对Pim-1和Pim-2的IC50分别为21nM和100nM，对其它50种激酶几乎无活性。
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AZD1208是口服活性的PIM高选择性抑制剂，对Pim1, Pim2, 和 Pim3的IC50分别为5 nM, 25 nM 和 16 nM。
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SGI-1776是ATP竞争性Pim1抑制剂，IC50为7 nM，比对Pim2和Pim3的抑制性高50倍和10倍，对Flt3和haspin也有抑制性。
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SMI-4a是ATP竞争性Pim激酶抑制剂，对Pim-1和Pim-2的IC50分别为21nM和100nM，对其它50种激酶几乎无活性。
More
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AZD1208是口服活性的PIM高选择性抑制剂，对Pim1, Pim2, 和 Pim3的IC50分别为5 nM, 25 nM 和 16 nM。
More
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SGI-1776是ATP竞争性Pim1抑制剂，IC50为7 nM，比对Pim2和Pim3的抑制性高50倍和10倍，对Flt3和haspin也有抑制性。
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