Pim
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
Pim产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2198 |
SGI-1776 free baseSGI-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。 |
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.
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| S8005 |
SMI-4aSMI-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。 |
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. |
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| S3296 |
HispidulinHispidulin (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。 |
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| S6497 |
SMI-16aSMI-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。 |
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| S1050 |
TCS PIM-1 1TCS PIM-1 1 (SC 204330)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）。 |
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| S8800 |
Uzansertib (INCB053914)Uzansertib (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。 |
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| S7985 |
PIM447 (LGH447)PIM447 (LGH447)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。 |
(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.
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| S7104 |
AZD1208AZD1208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。 |
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. |
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| S7041 |
CX-6258 HClCX-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。 |
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| S6774 |
TP-3654TP-3654是第二代 PIM 抑制剂，对于PIM-1、PIM-2和PIM-3的Ki值分别为5 nM、239 nM和42 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2198 |
SGI-1776 free baseSGI-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。 |
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-4aSMI-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。 |
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 |
HispidulinHispidulin (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-16aSMI-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。 |
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| S1050 |
TCS PIM-1 1TCS PIM-1 1 (SC 204330)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）。 |
||
| S8800 |
Uzansertib (INCB053914)Uzansertib (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。 |
||
| S7985 |
PIM447 (LGH447)PIM447 (LGH447)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。 |
(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.
|
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| S7104 |
AZD1208AZD1208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。 |
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 HClCX-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。 |
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| S6774 |
TP-3654TP-3654是第二代 PIM 抑制剂，对于PIM-1、PIM-2和PIM-3的Ki值分别为5 nM、239 nM和42 nM。 |
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