Pim

亜型選択性的な製品

Pim1 Pim2 Pim3

シグナル伝達経路

Pim製品

All (12)
Pim阻害剤 (12)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S2198	SGI-1776 free base	SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy.	Cell Death Dis, 2024, 15(9):644 Mol Cancer, 2023, 22(1):64 Int J Mol Sci, 2023, 24(6)5464
S7104	AZD1208	AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.	Angiogenesis, 2024, 10.1007/s10456-024-09906-y Cell Death Dis, 2024, 15(4):274 Inflamm Res, 2024, 10.1007/s00011-024-01924-2
S7985	PIM447 (LGH447) Hydrochloride	PIM447 (LGH447) Hydrochloride is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>10⁵-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis.	Oncogene, 2024, 43(6):406-419 NPJ Precis Oncol, 2024, 8(1):152 Antiviral Res, 2024, 226:105891
S8005	SMI-4a	SMI-4a (TCS PIM-1 4a) is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.	Transl Gastroenterol Hepatol, 2024, 9:14 J Transl Med, 2023, 21(1):452 Nat Commun, 2022, 13-1:5866
S7041	CX-6258 HCl	CX-6258 HCl is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.	Elife, 2023, 12e69521 Nat Med, 2020, 10.1038/s41591-020-0926-0 Nat Commun, 2020, 29;11(1):2086
S8800	Uzansertib (INCB053914)	Uzansertib (INCB053914) is a novel, ATP-competitive, small molecule, pan-inhibitor of PIM kinases with IC50 values of 0.24 nM, 30 nM and 0.12 nM for PIM1, PIM2 and PIM3 respectively in biochemical assays.	Antiviral Res, 2024, 226:105891 Cancer Lett, 2020, 476:23-33 Fish Shellfish Immunol, 2020, 99:86-98
S6774	TP-3654	TP-3654 is the second-generation PIM inhibitor with K_i values of 5 nM, 239 nM, and 42 nM for PIM-1, PIM-2 and PIM-3, respectively.	PLoS One, 2023, 10.1371/journal.pone.0294065 Int J Mol Sci, 2021, 22(17)9440
S3296	Hispidulin	Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.	Evid Based Complement Alternat Med, 2023, 2023:9428241
S6497	SMI-16a	SMI-16a is a selective Pim kinase inhibitor with IC50 values of 150 nM and 20 nM for Pim1 and Pim2 respectively.	J Cell Physiol, 2022, 10.1002/jcp.30814
E4598^New	MEN1703(SEL24,SEL24-B489)	MEN1703(SEL24-B489,SEL24, Pim/flt3 kinase inhibitor SEL24) is a potent, type I, orally active, dual inhibitor of PIM and FLT3-ITD, that exhibits Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively. MEN1703 exhibits its broad therapeutic potential in treatment of acute myeloid leukemia.
S1050	TCS PIM-1 1	TCS PIM-1 1 (SC 204330) is a potent and selective inhibitor of ATP-competitive Pim-1 kianse with IC50 of 50 nM, shows good selectivity over Pim-2 and MEK1/MEK2 with IC50 > 20000 nM.
E0675	Quercetagetin	Quercetagetin (6-Hydroxyquercetin), a flavonoid, is a moderately potent and selective, cell-permeable Pim-1 kinase inhibitor with IC50 of 0.34 μM.
S2198	SGI-1776 free base	SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy.	Cell Death Dis, 2024, 15(9):644 Mol Cancer, 2023, 22(1):64 Int J Mol Sci, 2023, 24(6)5464
S7104	AZD1208	AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.	Angiogenesis, 2024, 10.1007/s10456-024-09906-y Cell Death Dis, 2024, 15(4):274 Inflamm Res, 2024, 10.1007/s00011-024-01924-2
S7985	PIM447 (LGH447) Hydrochloride	PIM447 (LGH447) Hydrochloride is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>10⁵-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis.	Oncogene, 2024, 43(6):406-419 NPJ Precis Oncol, 2024, 8(1):152 Antiviral Res, 2024, 226:105891
S8005	SMI-4a	SMI-4a (TCS PIM-1 4a) is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.	Transl Gastroenterol Hepatol, 2024, 9:14 J Transl Med, 2023, 21(1):452 Nat Commun, 2022, 13-1:5866
S7041	CX-6258 HCl	CX-6258 HCl is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.	Elife, 2023, 12e69521 Nat Med, 2020, 10.1038/s41591-020-0926-0 Nat Commun, 2020, 29;11(1):2086
S8800	Uzansertib (INCB053914)	Uzansertib (INCB053914) is a novel, ATP-competitive, small molecule, pan-inhibitor of PIM kinases with IC50 values of 0.24 nM, 30 nM and 0.12 nM for PIM1, PIM2 and PIM3 respectively in biochemical assays.	Antiviral Res, 2024, 226:105891 Cancer Lett, 2020, 476:23-33 Fish Shellfish Immunol, 2020, 99:86-98
S6774	TP-3654	TP-3654 is the second-generation PIM inhibitor with K_i values of 5 nM, 239 nM, and 42 nM for PIM-1, PIM-2 and PIM-3, respectively.	PLoS One, 2023, 10.1371/journal.pone.0294065 Int J Mol Sci, 2021, 22(17)9440
S3296	Hispidulin	Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.	Evid Based Complement Alternat Med, 2023, 2023:9428241
S6497	SMI-16a	SMI-16a is a selective Pim kinase inhibitor with IC50 values of 150 nM and 20 nM for Pim1 and Pim2 respectively.	J Cell Physiol, 2022, 10.1002/jcp.30814
E4598^New	MEN1703(SEL24,SEL24-B489)	MEN1703(SEL24-B489,SEL24, Pim/flt3 kinase inhibitor SEL24) is a potent, type I, orally active, dual inhibitor of PIM and FLT3-ITD, that exhibits Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively. MEN1703 exhibits its broad therapeutic potential in treatment of acute myeloid leukemia.
S1050	TCS PIM-1 1	TCS PIM-1 1 (SC 204330) is a potent and selective inhibitor of ATP-competitive Pim-1 kianse with IC50 of 50 nM, shows good selectivity over Pim-2 and MEK1/MEK2 with IC50 > 20000 nM.
E0675	Quercetagetin	Quercetagetin (6-Hydroxyquercetin), a flavonoid, is a moderately potent and selective, cell-permeable Pim-1 kinase inhibitor with IC50 of 0.34 μM.
E4598^New	MEN1703(SEL24,SEL24-B489)	MEN1703(SEL24-B489,SEL24, Pim/flt3 kinase inhibitor SEL24) is a potent, type I, orally active, dual inhibitor of PIM and FLT3-ITD, that exhibits Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively. MEN1703 exhibits its broad therapeutic potential in treatment of acute myeloid leukemia.

Pim阻害剤の選択性比較