Pim

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研究领域

抑制剂选择性比较

特异性亚型抑制剂

Pim产品

所有产品 Pim抑制剂(10)

目录号	产品描述	文献引用	实验数据
S2198	SGI-1776 free base SGI-1776 free base是一种新型的，ATP竞争性Pim1抑制剂，无细胞试验中IC50为7 nM，比作用于Pim2和Pim3选择性分别高50和10倍，也有效作用于Flt3和haspin。SGI-1776 可诱导凋亡和自噬。Phase 1。	Haematologica, 2020, 28;haematol.2019.223529 Arterioscler Thromb Vasc Biol, 2020, 10.1161/ATVBAHA.119.313763 Mol Ther Oncolytics, 2020, 30;17:169-179	VCaP cells were steroid starved overnight then treated with 10nM R1881 and PIM kinase inhibitor SGI-1776 as indicated for 4 hours. Total protein lysates were analyzed by Western blot with antibodies against P-AR S213, AR (total), P-4EBP1 Thr 37/46, and tubulin.
S8005	SMI-4a SMI-4a (TCS PIM-1 4a) 是一种有效的Pim1抑制剂，IC50为17 nM，作用于Pim-2适度有效，抑制其他丝/苏氨酸或酪氨酸激酶作用不显著。	Haematologica, 2020, 28;haematol.2019.223529 Arthritis Rheumatol, 2019, 71(8):1308-1318 Int Immunopharmacol, 2019, 73:568-574	Loss of proliferation in ATL-derived cell lines by the Pim-kinase inhibitors, Smi-4a (C). Cell counts were repeated at least twice. Results represent the percentage of cells alive after 5 days of Pim inhibitor treatment, compared with 5 days treated with DMSO. For Smi-4a treatment, cells were treated with 0, 10, or 20 μM Smi-4a. Normal PBMCs (n = 2) were used as a control. Western blots indicate loss of Pim1 targets, p-4EBP1 (Thr37/46), p-p70S6K (Thr389), and loss of pBad (Ser20) (negligible for Smi-4a) after 24 hours with 0, 10, 20, or 40 μM Smi-4a or DMSO control.
S3296^New	Hispidulin Hispidulin (Dinatin) 是一种在许多传统中草药中存在的天然活性成分，对癌蛋白激酶 Pim-1 具有抑制活性，其IC50值为2.71 μM。Hispidulin 通过 mitochondrial dysfunction 来诱导凋亡，并可抑制HepG2癌细胞中的 P13k/Akt 的信号通路。Hispidulin 通过激活 AMPK 信号通路发挥抗骨质疏松和骨吸收减弱的作用。
S6497	SMI-16a SMI-16a是选择性Pim激酶抑制剂，对Pim1和Pim2的IC50值分别为150 nM和20 nM。
S1050^New	TCS PIM-1 1 TCS PIM-1 1 是一种有效的、选择性的 ATP-competitive Pim-1 kianse 抑制剂，其IC50值为50 nM，对 Pim-2 和 MEK1/MEK2 具有良好的选择性（IC50> 20000 nM）。
S6774^New	TP-3654 TP-3654是第二代 PIM 抑制剂，对于PIM-1、PIM-2和PIM-3的K_i值分别为5 nM、239 nM和42 nM。
S8800	INCB053914 INCB053914是一种新型的、ATP竞争性的PIM kinases抑制剂，对PIM1、PIM2、PIM3的IC50值分别为0.24 nM、30 nM和0.12 nM。	Cancer Lett, 2020, 476:23-33 Fish Shellfish Immunol, 2020, 99:86-98
S7985	PIM447 (LGH447) PIM447是一种新型的、泛PIM激酶抑制剂，对PIM1、PIM2、PIM3的Ki值分别为6 pM、18 pM、9 pM。它还能抑制 GSK3β, PKN1和PKCτ，但抑制效力较小，IC50在1-5 μM范围间。 PIM447 可诱导凋亡。	Haematologica, 2020, 28;haematol.2019.223529 Cell Death Dis, 2020, 20;11(4):255 Int J Mol Sci, 2020, 21(14):5138	(H) MV4-11 cells were treated for 6 hours with or without 3 ng/ml BZM, 10 μM PF, or 3 μM PIM, as indicated, and analyzed.
S7104	AZD1208 AZD1208是一种有效的口服可利用的Pim kinase抑制剂，在无细胞试验中对Pim1, Pim2, and Pim3的IC50分别为0.4 nM，5 nM，和 1.9 nM。AZD1208可诱导自噬、细胞周期阻滞和凋亡。Phase 1。	Haematologica, 2020, 28;haematol.2019.223529 Toxicol In Vitro, 2020, 62:104677 Blood Adv, 2020, 4(5):819-829	Loss of proliferation in ATL-derived cell lines by the Pim-kinase inhibitor AZD1208 (D). Cell counts were repeated at least twice. Results represent the percentage of cells alive after 5 days of Pim inhibitor treatment, compared with 5 days treated with DMSO. For AZD1208, cells were treated with 0, 5, or 10 μM AZD1208. Normal PBMCs (n = 2) were used as a control. Western blots indicate loss of Pim1 targets, p-4EBP1 (Thr37/46), p-p70S6K (Thr389), and loss of pBad (Ser20) (negligible for Smi-4a) after 24 hours with 0, 5, or 10 μM AZD1208; or DMSO control.
S7041	CX-6258 HCl CX-6258 HCl 是强效的可口服的pan-Pim kinase抑制剂，其对Pim1, Pim2, 和 Pim3的IC50分别为5 nM, 25 nM 和 16 nM。	Nat Med, 2020, 10.1038/s41591-020-0926-0 Nat Commun, 2020, 29;11(1):2086 Haematologica, 2020, 28;haematol.2019.223529

目录号	产品描述	文献引用	实验数据
S2198	SGI-1776 free base SGI-1776 free base是一种新型的，ATP竞争性Pim1抑制剂，无细胞试验中IC50为7 nM，比作用于Pim2和Pim3选择性分别高50和10倍，也有效作用于Flt3和haspin。SGI-1776 可诱导凋亡和自噬。Phase 1。	Haematologica,2020, 28;haematol.2019.223529 Arterioscler Thromb Vasc Biol,2020, 10.1161/ATVBAHA.119.313763 Mol Ther Oncolytics,2020, 30;17:169-179	VCaP cells were steroid starved overnight then treated with 10nM R1881 and PIM kinase inhibitor SGI-1776 as indicated for 4 hours. Total protein lysates were analyzed by Western blot with antibodies against P-AR S213, AR (total), P-4EBP1 Thr 37/46, and tubulin.
S8005	SMI-4a SMI-4a (TCS PIM-1 4a) 是一种有效的Pim1抑制剂，IC50为17 nM，作用于Pim-2适度有效，抑制其他丝/苏氨酸或酪氨酸激酶作用不显著。	Haematologica,2020, 28;haematol.2019.223529 Arthritis Rheumatol,2019, 71(8):1308-1318 Int Immunopharmacol,2019, 73:568-574	Loss of proliferation in ATL-derived cell lines by the Pim-kinase inhibitors, Smi-4a (C). Cell counts were repeated at least twice. Results represent the percentage of cells alive after 5 days of Pim inhibitor treatment, compared with 5 days treated with DMSO. For Smi-4a treatment, cells were treated with 0, 10, or 20 μM Smi-4a. Normal PBMCs (n = 2) were used as a control. Western blots indicate loss of Pim1 targets, p-4EBP1 (Thr37/46), p-p70S6K (Thr389), and loss of pBad (Ser20) (negligible for Smi-4a) after 24 hours with 0, 10, 20, or 40 μM Smi-4a or DMSO control.
S3296^New	Hispidulin Hispidulin (Dinatin) 是一种在许多传统中草药中存在的天然活性成分，对癌蛋白激酶 Pim-1 具有抑制活性，其IC50值为2.71 μM。Hispidulin 通过 mitochondrial dysfunction 来诱导凋亡，并可抑制HepG2癌细胞中的 P13k/Akt 的信号通路。Hispidulin 通过激活 AMPK 信号通路发挥抗骨质疏松和骨吸收减弱的作用。
S6497	SMI-16a SMI-16a是选择性Pim激酶抑制剂，对Pim1和Pim2的IC50值分别为150 nM和20 nM。
S1050^New	TCS PIM-1 1 TCS PIM-1 1 是一种有效的、选择性的 ATP-competitive Pim-1 kianse 抑制剂，其IC50值为50 nM，对 Pim-2 和 MEK1/MEK2 具有良好的选择性（IC50> 20000 nM）。
S6774^New	TP-3654 TP-3654是第二代 PIM 抑制剂，对于PIM-1、PIM-2和PIM-3的K_i值分别为5 nM、239 nM和42 nM。
S8800	INCB053914 INCB053914是一种新型的、ATP竞争性的PIM kinases抑制剂，对PIM1、PIM2、PIM3的IC50值分别为0.24 nM、30 nM和0.12 nM。	Cancer Lett,2020, 476:23-33 Fish Shellfish Immunol,2020, 99:86-98
S7985	PIM447 (LGH447) PIM447是一种新型的、泛PIM激酶抑制剂，对PIM1、PIM2、PIM3的Ki值分别为6 pM、18 pM、9 pM。它还能抑制 GSK3β, PKN1和PKCτ，但抑制效力较小，IC50在1-5 μM范围间。 PIM447 可诱导凋亡。	Haematologica,2020, 28;haematol.2019.223529 Cell Death Dis,2020, 20;11(4):255 Int J Mol Sci,2020, 21(14):5138	(H) MV4-11 cells were treated for 6 hours with or without 3 ng/ml BZM, 10 μM PF, or 3 μM PIM, as indicated, and analyzed.
S7104	AZD1208 AZD1208是一种有效的口服可利用的Pim kinase抑制剂，在无细胞试验中对Pim1, Pim2, and Pim3的IC50分别为0.4 nM，5 nM，和 1.9 nM。AZD1208可诱导自噬、细胞周期阻滞和凋亡。Phase 1。	Haematologica,2020, 28;haematol.2019.223529 Toxicol In Vitro,2020, 62:104677 Blood Adv,2020, 4(5):819-829	Loss of proliferation in ATL-derived cell lines by the Pim-kinase inhibitor AZD1208 (D). Cell counts were repeated at least twice. Results represent the percentage of cells alive after 5 days of Pim inhibitor treatment, compared with 5 days treated with DMSO. For AZD1208, cells were treated with 0, 5, or 10 μM AZD1208. Normal PBMCs (n = 2) were used as a control. Western blots indicate loss of Pim1 targets, p-4EBP1 (Thr37/46), p-p70S6K (Thr389), and loss of pBad (Ser20) (negligible for Smi-4a) after 24 hours with 0, 5, or 10 μM AZD1208; or DMSO control.
S7041	CX-6258 HCl CX-6258 HCl 是强效的可口服的pan-Pim kinase抑制剂，其对Pim1, Pim2, 和 Pim3的IC50分别为5 nM, 25 nM 和 16 nM。	Nat Med,2020, 10.1038/s41591-020-0926-0 Nat Commun,2020, 29;11(1):2086 Haematologica,2020, 28;haematol.2019.223529