Pim

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Pim1	Pim2	Pim3	Other
A10838	SGI-1776 free base	***	*	*	FLT3
A11945	SMI-4a	**
A14275	CX-6258 HCl	***	**	**
A13203	AZD1208	****	***	****
A11967	TCS PIM-1 4a	**	*
A12896	CX-6258	***	**	**
A15368	PIM-1 Inhibitor 2	*
A15369	TCS PIM-1 1	*

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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SGI-1776 (free base)

Catalog No. A10838
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PIM1 抑制剂

SGI-1776 (free base)是Pim1的一种新型ATP竞争性抑制剂，在无细胞试验中的IC50为7 nM，选择性是Pim2和Pim3的50倍和10倍，对Flt3和haspin也有效。阶段1。了解更多

Product Citations (1)

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- Ishikawa C, .et al. Expression and significance of Pim-3 kinase in adult T-cell leukemia, Eur J Haematol, 2017, Dec;99(6):495-504 PMID: 28833639
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LGB-321 HCl

Catalog No. A14420
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Pan-PIM kinase 抑制剂

LGB-321 HCl是一种有效且选择性的PIM激酶竞争性小分子抑制剂（Pan-PIM激酶抑制剂）。了解更多

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- Andrea L. Casillas, .et al. Hypoxia-inducible PIM kinase expression promotes resistance to anti-angiogenic agents, Clin Cancer Res, 2018, Jan 1; 24(1): 169-180 PMID: 29084916
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AZD1208

Catalog No. A13203
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pan-Pim kinase 抑制剂

AZD1208是PIM激酶的小分子抑制剂，具有潜在的抗肿瘤活性。了解更多

Product Citations (5)

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- Remy J, .et al. Inhibition of PIM1 blocks the autophagic flux to sensitize glioblastoma cells to ABT-737-induced apoptosis, Biochim Biophys Acta Mol Cell Res, 2019, Feb;1866(2):175-189 PMID: 30389373
- Andrea L. Casillas, .et al. Hypoxia-inducible PIM kinase expression promotes resistance to anti-angiogenic agents, Clin Cancer Res, 2018, Jan 1; 24(1): 169-180 PMID: 29084916
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
- Sathish K.R. Padi, .et al. Targeting the PIM protein kinases for the treatment of a T-cell acute lymphoblastic leukemia subset, Oncotarget, 2017, May 2; 8(18): 30199-30216 PMID: 28415816
- Lim R, .et al. Inhibition of PIM1 kinase attenuates inflammation-induced pro-labour mediators in human foetal membranes in vitro, Mol Hum Reprod, 2017, Jun 1;23(6):428-440 PMID: 28333279
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CX-6258 HCl

Catalog No. A14275
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Pan-PIM kinase 抑制剂

CX-6258 HCl是一种有效的口服泛Pim激酶抑制剂，对Pim1，Pim2和Pim3的IC50为5 nM，25 nM和16 nM。了解更多

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TCS PIM-1 4a (SMI-4a)

Catalog No. A11967
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Pim 抑制剂

TCS PIM-1 4a (SMI-4a)是一种具有选择性和ATP竞争性的Pim激酶抑制剂（Pim-1和Pim-2的IC50值分别为24和100 nM）。了解更多

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PIM-1 Inhibitor 2

Catalog No. A15368
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PIM-1 抑制剂

PIM-1 Inhibitor 2 是有效的Pim-1激酶抑制剂（Ki = 91 nM）。了解更多

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CX-6258

Catalog No. A12896
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Pim 抑制剂

CX-6258是一种有效，选择性和口服有效的pan-Pim激酶抑制剂。了解更多

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TCS PIM-1 1

Catalog No. A15369
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Pim-1 Kinase 抑制剂

TCS PIM-1 1是一种有效的且具有选择性的ATP竞争性Pim-1 kianse抑制剂，IC50为50 nM，对Pim-2和MEK1/MEK2表现出良好的选择性（IC50s> 20,000 nM）。了解更多

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CX-6258 hydrochloride hydrate

Catalog No. A15055
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Pim 抑制剂

CX-6258 hydrochloride hydrate是一种有效的，口服有效的Pim 1/2/3激酶（IC50 = 5 nM/25 nM/16 nM）抑制剂，具有出色的生化效能和激酶选择性。了解更多

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