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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(Z)-SMI-4a

Catalog No. A11945
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Pim 抑制剂

SIM-4a是一种Pim激酶抑制剂，可通过激活AMPK来阻断mTORC1的活性。通常对Pim-2有效，不会显着抑制任何其他丝氨酸/苏氨酸或酪氨酸激酶。了解更多

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- Liong S, .et al. Placental Pim-1 expression is increased in obesity and regulates cytokine- and toll-like receptor-mediated inflammation, Placenta, 2017, May;53:101-112 PMID: 28487013
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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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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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TP-3654

Catalog No. A20584
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Pim kinase inhibitor

TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively. 了解更多

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PIM1-IN-1

Catalog No. A19392
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PIM1/3 inhibitor

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. 了解更多

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GNE-955

Catalog No. A19243
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Pim kinase inhibitor

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. 了解更多

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INCB053914 phosphate

Catalog No. A21444
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Pim inhibitor

INCB053914 phosphate is an inhibitor of Pim extracted from patent WO 2017044730 A1, compound 1; has an IC50 of less than 35 nM. 了解更多

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GDC-0339

Catalog No. A20920
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Pim kinase inhibitor

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. 了解更多

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- 最新产品
SMI-16a

Catalog No. A17157
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Pim kinase 抑制剂

SMI-16a是选择性的Pim激酶抑制剂，其对Pim1，Pim2和PC3细胞的IC 50值分别为0.15、0.02和48μM。了解更多

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PIM447 (LGH447)

Catalog No. A16807
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Pim 抑制剂

PIM447 (LGH447)是一种新型的pan-PIM激酶抑制剂，其PIM1，PIM2，PIM3的Ki值分别为6 pM，18 pM，9 pM。它也抑制GSK3β，PKN1和PKCτ，但效力显着降低，IC50在1-5μM之间（相对于PIM上Ki的差异> 105倍）。了解更多

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AZD1208 HCl

Catalog No. A16927
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PIM kinases 抑制剂

AZD1208 HCl是一种新型的，口服可生物利用的高选择性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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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 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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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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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 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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