BX 912
BX-912
CAS: 702674-56-4
Molecular Formula: C20H23BrN8O
BX 912 - Names and Identifiers
BX 912 - Physico-chemical Properties
| Molecular Formula | C20H23BrN8O |
| Molar Mass | 471.35 |
| Density | 1.596 |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | -20°C |
| Use | A potent and selective PDK-1 inhibitor that induces apoptosis |
| In vitro study | BX912 inhibited ChcK1,PKA,c-kit, and KDR with IC50 of 0.83, 0.11, 0.85, and 0.41 μm, respectively. BX912 acts on tumor cells, blocks PDK1/Akt signaling, and also inhibits the Anchorage-dependent growth of various tumor cells (such as PC-3 cells) or induces apoptosis in culture. Many cancer cell lines (such as MDA-468 breast cancer) have increased Akt activity, and tissues cultured in soft agar are more than 30 times more sensitive to BX912 than tissue culture plastic, consistent with cell survival in the PDK1/Akt signaling pathway, this is especially important for non-adherent cells. BX912 effectively inhibited PDK1 enzyme activity, but did not inhibit AKT2 activity (IC50>10 μm). Thus, BX-912 is a direct inhibitor of pdk1. BX912 is a competitive inhibitor of PDK1 activity, and BX912 binds to the ATP-binding pocket of pdk1. The aminopyrimidine backbone of BX912 employs a site similar to the PDK1 activation site. BX912 significantly increased the number of MDA-468 cells containing 4 N DNA and allowed the cells to stop at G2/M phase. BX912 also effectively inhibited the growth of HCT-116 cells, and the inhibition rate was 96% at the dose of 1 μm. BX912 effectively inhibited cell growth with an IC50 of 0.32 μm. BX912 inhibits ChcK1,PKA,c-kit, and KDR with IC50 of 0.83, 0.11, 0.85, and 0.41 μm, respectively. BX912 acts on tumor cells, blocks PDK1/Akt signaling, and also inhibits the Anchorage-dependent growth of various tumor cells (such as PC-3 cells) or induces apoptosis in culture. Many cancer cell lines (such as MDA-468 breast cancer) have increased Akt activity, and tissues cultured in soft agar are more than 30 times more sensitive to BX912 than tissue culture plastic, consistent with cell survival in the PDK1/Akt signaling pathway, this is especially important for non-adherent cells. BX912 effectively inhibited PDK1 enzyme activity, but did not inhibit AKT2 activity (IC50>10 μm). Thus, BX-912 is a direct inhibitor of pdk1. BX912 is a competitive inhibitor of PDK1 activity, and BX912 binds to the ATP-binding pocket of pdk1. The aminopyrimidine backbone of BX912 employs a site similar to the PDK1 activation site. BX912 significantly increased the number of MDA-468 cells containing 4 N DNA and allowed the cells to stop at G2/M phase. BX912 also effectively inhibited the growth of HCT-116 cells, and the inhibition rate was 96% at the dose of 1 μm. BX912 effectively inhibited cell growth with an IC50 of 0.32 μm. |
BX 912 - Risk and Safety
| WGK Germany | 3 |
BX 912 - Introduction
BX-912 is an effective and specific PDK1 inhibitor with an IC50 of 12 nM. The selectivity of PKD1 is 9 and 105 times higher than that of PKA and PKC respectively.
Last Update：2022-10-16 17:28:04
BX 912 - Reference Information
| biological activity | BX-912 is an effective and specific PDK1 inhibitor with IC50 of 12 nM, and its selectivity to PKD1 is 9 and 105 times higher than that to PKA and PKC respectively. BX-912 is an effective and specific PDK1 inhibitor. IC50 is 12 nM in cell-free test. the selectivity of PDK1 is 9 and 105 times higher than that of PKA and PKC respectively. Compared with GSK3β, the selectivity for PDK1 is 600 times. |
| in vitro study | BX912 inhibited ChcK1,PKA,c-kit, and KDR,IC50 by 0.83, 0.11, 0.85, and 0.41 μM respectively. BX912 acts on tumor cells to block PDK1/Akt signal, and also inhibits the adherent growth of various tumor cells (such as PC-3 cells) or induces apoptosis in culture. Many cancer cell lines (such as MDA-468 breast cancer) have increased Akt activity. The sensitivity of tissues cultured in soft agar to BX912 is more than 30 times higher than that on tissue culture plastic, and the cell survival of PDK1/Akt signaling pathway is consistent, which is especially important for cells without adhesion. BX912 effectively inhibited PDK1 activity, but did not inhibit AKT2 activity (IC50>10 μM). Therefore, BX-912 is a direct inhibitor of PDK1. BX912 is a competitive inhibitor of PDK1 activity, and BX912 binds to the ATP-binding bag of PDK1. The aminopyrimidine skeleton of BX912 adopts a site similar to the PDK1 activation site. BX912 significantly increased the number of MDA-468 cells containing 4 N DNA and stopped the cells in G2/M phase. BX912 also effectively inhibited the growth of HCT-116 cells, with an inhibition rate of 96% treated at a dose of 1 μM. BX912 effectively inhibited cell growth with IC50 of 0.32 μM. BX912 inhibited ChcK1,PKA,c-kit, and KDR,IC50 of 0.83, 0.11, 0.85, and 0.41 μM respectively. BX912 acts on tumor cells to block PDK1/Akt signal, and also inhibits the adherent growth of various tumor cells (such as PC-3 cells) or induces apoptosis in culture. Many cancer cell lines (such as MDA-468 breast cancer) have increased Akt activity. The sensitivity of tissues cultured in soft agar to BX912 is more than 30 times higher than that on tissue culture plastic, and the cell survival of PDK1/Akt signaling pathway is consistent, which is especially important for cells without adhesion. BX912 effectively inhibited PDK1 activity, but did not inhibit AKT2 activity (IC50>10 μM). Therefore, BX-912 is a direct inhibitor of PDK1. BX912 is a competitive inhibitor of PDK1 activity, and BX912 binds to the ATP-binding bag of PDK1. The aminopyrimidine skeleton of BX912 adopts a site similar to the PDK1 activation site. BX912 significantly increased the number of MDA-468 cells containing 4 N DNA and stopped the cells in G2/M phase. BX912 also effectively inhibited the growth of HCT-116 cells, with an inhibition rate of 96% treated at a dose of 1 μM. BX912 effectively inhibited cell growth with IC50 of 0.32 μM. |
| target | TargetValue PDK-1 12 nM PKA (Cell-Free Assay) 110 nM KDR (Cell-Free Assay) 410 nM CDK2/CyclinE (Cell-Free Assay) 650 nM Chk1 (Cell-Free Assay) 830 nM |
| Target | Value |
| PDK-1 (Cell-free assay) | 12 nM |
| PKA (Cell-free assay) | 110 nM |
| KDR (Cell-free assay) | 410 nM |
| CDK2/CyclinE (Cell-free assay) | 650 nM |
| Chk1 (Cell-free assay) | 830 nM |
Last Update：2024-04-09 20:52:54
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CAS: 702674-56-4
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CAS: 702674-56-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: BX-912 Visit Supplier Webpage Request for quotation
CAS: 702674-56-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 702674-56-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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