Pim

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Catalog No. Product Name Information Product Use Citations Product Validations
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.
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. Phase 1.
Cancer Res, 2021, canres.1023.2021
Commun Biol, 2021, 4(1):1221
Cell, 2020, 182(3):685-712.e19
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.
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.
S6774 TP-3654 TP-3654 is the second-generation PIM inhibitor with Ki values of 5 nM, 239 nM, and 42 nM for PIM-1, PIM-2 and PIM-3, respectively.
Int J Mol Sci, 2021, 22(17)9440
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.
Nat Med, 2020, 10.1038/s41591-020-0926-0
Nat Commun, 2020, 29;11(1):2086
Haematologica, 2020, 28;haematol.2019.223529
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.
Blood, 2022, blood.2021014011
Cell Rep, 2021, 35(8):109160
Cancers (Basel), 2021, 13(9)2139
S7985 PIM447 (LGH447) PIM447 (LGH447) 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.
Cancer Res, 2021, canres.1023.2021
J Pediatr Surg, 2021, S0022-3468(21)00173-1
Chem Pharm Bull (Tokyo), 2021, 69(9):854-861
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.
Haematologica, 2020, 28;haematol.2019.223529
Inflamm Res, 2020, 10.1007/s00011-020-01420-3
Arthritis Rheumatol, 2019, 71(8):1308-1318
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.
Cancer Lett, 2020, 476:23-33
Fish Shellfish Immunol, 2020, 99:86-98
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.
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. Phase 1.
Cancer Res, 2021, canres.1023.2021
Commun Biol, 2021, 4(1):1221
Cell, 2020, 182(3):685-712.e19
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.
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.
S6774 TP-3654 TP-3654 is the second-generation PIM inhibitor with Ki values of 5 nM, 239 nM, and 42 nM for PIM-1, PIM-2 and PIM-3, respectively.
Int J Mol Sci, 2021, 22(17)9440
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.
Nat Med, 2020, 10.1038/s41591-020-0926-0
Nat Commun, 2020, 29;11(1):2086
Haematologica, 2020, 28;haematol.2019.223529
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.
Blood, 2022, blood.2021014011
Cell Rep, 2021, 35(8):109160
Cancers (Basel), 2021, 13(9)2139
S7985 PIM447 (LGH447) PIM447 (LGH447) 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.
Cancer Res, 2021, canres.1023.2021
J Pediatr Surg, 2021, S0022-3468(21)00173-1
Chem Pharm Bull (Tokyo), 2021, 69(9):854-861
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.
Haematologica, 2020, 28;haematol.2019.223529
Inflamm Res, 2020, 10.1007/s00011-020-01420-3
Arthritis Rheumatol, 2019, 71(8):1308-1318
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.
Cancer Lett, 2020, 476:23-33
Fish Shellfish Immunol, 2020, 99:86-98