2-(3,5-Difluoro-4-hydroxyphenylamino)-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydro-5H-pteridin-6-one
BI-D1870
CAS: 501437-28-1
Molecular Formula: C19H23F2N5O2
2-(3,5-Difluoro-4-hydroxyphenylamino)-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydro-5H-pteridin-6-one - Names and Identifiers
2-(3,5-Difluoro-4-hydroxyphenylamino)-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydro-5H-pteridin-6-one - Physico-chemical Properties
| Molecular Formula | C19H23F2N5O2 |
| Molar Mass | 391.42 |
| Density | 1.297 |
| Boling Point | 579.3±60.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to 15 mg/ml) |
| Appearance | Off-white solid. |
| Color | Off-white |
| pKa | 7.68±0.36(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Use | BI-D1870 is an ATP-competitive S6 ribosome inhibitor that acts on RSK1/2/3/K4 with IC50 of 31 nM/24 nM/18 nM/15 nM, respectively. The selectivity of RSK is 10 to 100 times higher than that of MST2, GSK-3β, MARK3, CK1 and Aurora B. |
| In vitro study | BI-D1870 inhibition of RSK1,RSK2,RSK3 and RSK4,IC50 10-30 nM, but at 100-fold higher concentrations, there was also no significant inhibition of 10 other AGC kinase members and more than 40 other protein kinases. BI-D1870 cell-permeable, acting on human embryonic kidney 293 cells and rat -2 cells, inhibited RSK-mediated phorbol ester and EGF-induced phosphorylation of glycogen synthase kinase-3β and lkb1. BI-D1870 acts on six other AGC kinases without affecting agonist-triggered substrate phosphorylation. Furthermore, BI-D1870 did not inhibit phorbol ester or EGF-induced CREB phosphorylation. BI-D1870 inhibition of RSK1,RSK2,RSK3 and RSK4 with an IC50 of 10-30 nM, but at 100-fold higher concentrations, there was also no significant inhibition of 10 other AGC kinase members and more than 40 other protein kinases. BI-D1870 cell-permeable, acting on human embryonic kidney 293 cells and rat -2 cells, inhibited RSK-mediated phorbol ester and EGF-induced phosphorylation of glycogen synthase kinase-3β and lkb1. BI-D1870 acts on six other AGC kinases without affecting agonist-triggered substrate phosphorylation. Furthermore, BI-D1870 did not inhibit phorbol ester or EGF-induced CREB phosphorylation. |
2-(3,5-Difluoro-4-hydroxyphenylamino)-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydro-5H-pteridin-6-one - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.555 ml | 12.774 ml | 25.548 ml |
| 5 mM | 0.511 ml | 2.555 ml | 5.11 ml |
| 10 mM | 0.255 ml | 1.277 ml | 2.555 ml |
| 5 mM | 0.051 ml | 0.255 ml | 0.511 ml |
Last Update：2024-01-02 23:10:35
2-(3,5-Difluoro-4-hydroxyphenylamino)-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydro-5H-pteridin-6-one - Reference Information
| biological activity | BI-D1870 is an ATP-competitive S6 ribosome inhibitor, which acts on RSK1/2/3/K4,IC50 is 31 nM/24 nM/18 nM/15 nM respectively, and the selectivity of RSK is 10 to 100 times higher than that of MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 is an ATP-competitive S6 ribosome inhibitor, which acts on RSK1/2/3/K4 and IC50 is 31 nM/24 nM/18 nM/15 nM respectively in cell-free test. the selectivity of RSK is 10 to 100 times higher than that of MST2,GSK-3β,MARK3,CK1 and Aurora B. BI-D1870 show that in addition to anti-cancer properties include the generation of reactive oxygen species, the improvement of endoplasmic reticulum stress response and the induction of autophagy. |
| in vitro study | BI-D1870 inhibit RSK1,RSK2,RSK3 and RSK4,IC50 is 10-30 nM, but at a higher concentration of 100 times, it does not significantly inhibit 10 other AGC kinase members and more than 40 other protein kinases. BI-D1870 permeable cells, acting on human embryonic kidney 293 cells and rat -2 cells, can inhibit RSK-mediated phosphorylation of glycogen synthase kinase-3β and LKB1 induced by phorbol ester and EGF. BI-D1870 acts on six other AGC kinases and does not affect the substrate phosphorylation triggered by the agonist. Moreover, BI-D1870 did not inhibit the phosphorylation of CREB induced by phorbol ester or EGF. BI-D1870 inhibits RSK1,RSK2,RSK3 and RSK4,IC50 is 10-30 nM, but at a higher concentration of 100 times, it does not significantly inhibit 10 other AGC kinase members and more than 40 other protein kinases. BI-D1870 permeable cells, acting on human embryonic kidney 293 cells and rat -2 cells, can inhibit RSK-mediated phosphorylation of glycogen synthase kinase-3β and LKB1 induced by phorbol ester and EGF. BI-D1870 acts on six other AGC kinases and does not affect the substrate phosphorylation triggered by the agonist. Moreover, BI-D1870 did not inhibit the phosphorylation of CREB induced by phorbol ester or EGF. |
| target | TargetValue rsk4 (cell-free assay) 15 nm rsk3 (cell-free assay) 18 nm rsk2 (cell-free assay) 24 nm rsk1 (cell-free assay) 31 nm |
| Target | Value |
| RSK4 (Cell-free assay) | 15 nM |
| RSK3 (Cell-free assay) | 18 nM |
| RSK2 (Cell-free assay) | 24 nM |
| RSK1 (Cell-free assay) | 31 nM |
Last Update：2024-04-09 20:49:11
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Spot supply
Product Name: BI-D1870 Visit Supplier Webpage Request for quotationCAS: 501437-28-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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