N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide BX-795
BX-795 盐酸盐
CAS: 702675-74-9
Molecular Formula: C23H26IN7O2S
N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide BX-795 - Names and Identifiers
N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide BX-795 - Physico-chemical Properties
| Molecular Formula | C23H26IN7O2S |
| Molar Mass | 591.47 |
| Density | 1.644 |
| Melting Point | >163°C (dec.) |
| Solubility | DMSO: soluble15mg/mL, clear |
| Appearance | powder |
| Color | white to light brown |
| pKa | 12.57±0.70(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Use | An inhibitor of PDK1, TBK1, and IKK&epsilon |
| In vitro study | BX795 also inhibited MARK1,MARK2,MARK4,NUAK1,VEGFR,MLK1,MLK2, and MLK3 with IC50 of 55,53,19,5,157,50,46, and 42 nM, respectively. 1 μm BX795 did not inhibit the following tyrosine protein kinases: hepatin receptors A2 and B3,Syk,Bruton's tyrosine kinase, and FGFR1. However, BX795 inhibits VEGFR with a lower inhibitory effect than TBK1. BX795 inhibits TBK1-catalyzed phosphorylation of IRF3 at the Ser396 site, which decreases with increasing ATP concentration, indicating that BX795 is a competitive inhibitor of ATP. BX795 blocks TBK1 and ikkε-regulated IRF3 activation and inhibits IFN-β production. After Poly (I:C) treatment, IRF3 accumulates in the nucleus, but can be inhibited by bx795. BX795 inhibits irf3-dependent gene transcription. BX795 inhibits the secretion of IFN-β from macrophages. BX795 had no effect on LPS-stimulated phosphorylation of p70 ribosomal S6 kinase 1 at the Thr229 site, which is the target of PDK1. BX795 does not affect the activation of ikkα/β complex or LPS, poly (I:C),IL-1α, or TNFα-promoted NFκB-dependent gene transcription. BX795 acts on IL-1α or TNFα-stimulated MEFs and also blocks JNK1/2 and p38α MAPK phosphorylation. Inhibition of TBK1/IKK ε by BX795 does not result in activation of JNK1/2 and p38α MAPK. BX795 also inhibits MARK1,MARK2,MARK4,NUAK1,VEGFR,MLK1,MLK2, and MLK3 with IC50 of 55,53,19,5,157,50,46 and 42 nM. 1 μm BX795 did not inhibit the following tyrosine protein kinases: hepatin receptors A2 and B3,Syk,Bruton's tyrosine kinase, and FGFR1. However, BX795 inhibits VEGFR with a lower inhibitory effect than TBK1. BX795 inhibits TBK1-catalyzed phosphorylation of IRF3 at the Ser396 site, which decreases with increasing ATP concentration, indicating that BX795 is a competitive inhibitor of ATP. BX795 blocks TBK1 and ikkε-regulated IRF3 activation and inhibits IFN-β production. After Poly (I:C) treatment, IRF3 accumulates in the nucleus, but can be inhibited by bx795. BX795 inhibits irf3-dependent gene transcription. BX795 inhibits the secretion of IFN-β from macrophages. BX795 had no effect on LPS-stimulated phosphorylation of p70 ribosomal S6 kinase 1 at the Thr229 site, which is the target of PDK1. BX795 does not affect the activation of ikkα/β complex or LPS, poly (I:C),IL-1α, or TNFα-promoted NFκB-dependent gene transcription. BX795 acts on IL-1α or TNFα-stimulated MEFs and also blocks JNK1/2 and p38α MAPK phosphorylation. Inhibition of TBK1/IKK ε by BX795 does not result in activation of JNK1/2 and p38α MAPK. |
N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide BX-795 - Risk and Safety
| WGK Germany | 3 |
N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide BX-795 - Introduction
BX-795 is an effective and specific PDK1 inhibitor with an IC50 of 6 nM. The selectivity of PDK1 is 140 and 1600 times higher than that of PKA and PKC, respectively.
Last Update：2022-10-16 17:41:46
N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide BX-795 - Reference Information
| biological activity | BX-795 is an effective and specific PDK1 inhibitor with IC50 of 6 nM. the selectivity for PDK1 is 140 and 1600 times higher than for PKA and PKC respectively. BX-795 is an effective and specific PDK1 inhibitor. IC50 is 6 nM in cell-free test. the selectivity of PDK1 is 140 and 1600 times higher than that of PKA and PKC respectively. At the same time, compared with GSK3β, the selectivity for PDK1 is more than 100 times higher. BX-795 can regulate autophagy by inhibiting ULK1. |
| in vitro studies | BX795 also inhibited MARK1,MARK2,MARK4,NUAK1,VEGFR,MLK1,MLK2, and MLK3,IC50 were 55,53,19,5,157,50,46 and 42 nM respectively. 1 μM BX795 does not inhibit the following tyrosine protein kinases: hepatic ligand receptors A2 and B3,Syk,Bruton's tyrosine kinase, and FGFR1. However, BX795 inhibits VEGFR and has a lower inhibitory effect than TBK1. BX795 inhibits TBK1-catalyzed phosphorylation of IRF3 at Ser396 site and decreases with increasing ATP concentration, indicating that BX795 is a competitive inhibitor of ATP. BX795 blocked the activation of IRF3 regulated by TBK1 and IKKε, and inhibited the production of IFN-β. After poly (I:C) treatment, IRF3 accumulates in the nucleus, but can be inhibited by BX795. BX795 inhibits IRF3-dependent gene transcription. BX795 inhibits IFN-β secretion from macrophages. BX795 has no effect on phosphorylation of p70 ribosomal S6 kinase 1 stimulated by LPS at Thr229 site, which is the target of PDK1. BX795 does not affect the activation of the IKKα/β complex or LPS, poly (I:C),IL-1α, or TNFα-promoted NFκB-dependent gene transcription. BX795 acts on IL-1α or TNFα-stimulated MEFs, also blocking JNK1/2 and p38α MAPK phosphorylation. BX795 inhibition of TBK1/IKKε did not lead to the activation of JNK1/2 and p38α MAPK. BX795 also inhibited MARK1,MARK2,MARK4,NUAK1,VEGFR,MLK1,MLK2, and MLK3,IC50 of 55,53,19,5,157,50,46 and 42 nM respectively. 1 μM BX795 does not inhibit the following tyrosine protein kinases: hepatic ligand receptors A2 and B3,Syk,Bruton's tyrosine kinase, and FGFR1. However, BX795 inhibits VEGFR and has a lower inhibitory effect than TBK1. BX795 inhibits TBK1-catalyzed phosphorylation of IRF3 at Ser396 site and decreases with increasing ATP concentration, indicating that BX795 is a competitive inhibitor of ATP. BX795 blocked the activation of IRF3 regulated by TBK1 and IKKε, and inhibited the production of IFN-β. After poly (I:C) treatment, IRF3 accumulates in the nucleus, but can be inhibited by BX795. BX795 inhibits IRF3-dependent gene transcription. BX795 inhibits IFN-β secretion from macrophages. BX795 has no effect on phosphorylation of p70 ribosomal S6 kinase 1 stimulated by LPS at Thr229 site, which is the target of PDK1. BX795 does not affect the activation of the IKKα/β complex or LPS, poly (I:C),IL-1α, or TNFα-promoted NFκB-dependent gene transcription. BX795 acts on IL-1α or TNFα-stimulated MEFs, also blocking JNK1/2 and p38α MAPK phosphorylation. BX795 inhibition of TBK1/IKKε did not lead to the activation of JNK1/2 and p38α MAPK. |
| target | TargetValue PDK-1 (Cell-free assay) 6 nM c-Kit (Cell-free assay) 320 nM CDK2/CyclinE (Cell-free assay) 430 nM Chk1 (Cell-free assay) 510 nM |
| Target | Value |
| PDK-1 (Cell-free assay) | 6 nM |
| c-Kit (Cell-free assay) | 320 nM |
| CDK2/CyclinE (Cell-free assay) | 430 nM |
| Chk1 (Cell-free assay) | 510 nM |
Last Update：2024-04-09 19:05:04
![N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide BX-795](http://res.chembk.com/assets/images/structure/309953.gif)
Supplier List
Spot supply
Product Name: BX-795 盐酸盐 Visit Supplier Webpage Request for quotationCAS: 702675-74-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: BX-795 盐酸盐 Visit Supplier Webpage Request for quotationCAS: 702675-74-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History