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.
Products for Pim
- Cat.No. 产品名称 Information
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GC34964
(1S,3R,5R)-PIM447 dihydrochloride
(1S,3R,5R)-LGH447 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。 -
GC12660
AZD1208
AZD 1208;AZD-1208
AZD1208 是一种有效、高选择性且可口服的 Pim 激酶抑制剂,对 PIM1、PIM2 和 PIM3 的 IC50 值分别为 0.4、5 和 1.9nM。 - GC35447 AZD1208 hydrochloride A pan-Pim kinase inhibitor
- GC39485 CK2/ERK8-IN-1 A dual inhibitor of CK2 and ERK8
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GC13056
CX-6258
CX6258;CX 6258
A pan-Pim kinase inhibitor -
GC19747
CX-6258 HCl
Pim-Kinase Inhibitor X
A pan-Pim kinase inhibitor -
GC35762
CX-6258 hydrochloride hydrate
(3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-1,4-二氮杂卓-1-基)羰基]苯基]-2-呋喃基]亚甲基]-1,3-二氢-2H-吲哚-2-酮盐酸盐水合物
A pan-Pim kinase inhibitor - GC32958 GDC-0339 GDC-0339是Pim激酶抑制剂,作用于BaF3PIM1时,IC50为43.6nM。
- GC33253 GNE-955 GNE-955是有效的泛Pim激酶抑制剂,Ki分别为18,110,8nM。
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GC12359
Hispidulin
高车前素; Dinatin
A flavonoid with diverse biological activities -
GC13154
LKB1(AAK1 dual inhibitor)
N-[5-(4-氰基苯基)-1H-吡咯并[2,3-B]吡啶-3-基]-3-吡啶甲酰胺,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。 - 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。
- GC49412 NSC 756093 An inhibitor of the GBP1-Pim-1 protein-protein interaction
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GC19419
PIM inhibitor 1 phosphate
INCB053914 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。 -
GC13558
PIM-1 Inhibitor 2
PIMi II
A potent PIM-1 kinase inhibitor -
GC36918
PIM-447 dihydrochloride
LGH447 dihydrochloride
PIM447是泛PIM激酶抑制剂,对PIM1,PIM2,PIM3的 Ki 分别为6,18,9 nM。 - 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。
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GC19398
PIM447
LGH447
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。 -
GC65201
Quercetagetin
六羟黄酮/栎草亭,6-Hydroxyquercetin
A selective Pim-1 inhibitor - 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。
- 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。
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GC16497
SGI-1776 free base
SGI1776,SGI 1776
A potent inhibitor of Pim kinases -
GC37651
SMI-16a
PIM1/2 Kinase Inhibitor VI
A Pim-1 kinase inhibitor - GC11104 SMI-4a A Pim kinase inhibitor
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GC17178
TCS PIM-1 1
SC 204330
A Pim-1 kinase inhibitor -
GC11990
TCS-PIM-1-4a
5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮,SMI-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)。 - GC19361 TP-3654 A Pim kinase inhibitor