BI-D1870
- CAS No.
- 501437-28-1
- Chemical Name:
- BI-D1870
- Synonyms
- CS-606;BI-D1870;BID1870;BI-D 1870;BI-D1870 USP/EP/BP;BI-D1870 RSK Inhibitor II;2-(3,5-Difluoro-4-hydroxyphenylamino)-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydro-5H-pteridin-6-one;2-[(3,5-DIFLUORO-4-HYDROXYPHENYL)AMINO]-7,8-DIHYDRO-5,7-DIMETHYL-8-(3-METHYLBUTYL)-6(5H)-PTERIDINONE;6(5H)-Pteridinone, 2-[(3,5-difluoro-4-hydroxyphenyl)amino]-7,8-dihydro-5,7-dimethyl-8-(3-methylbutyl)-;2-[(3,5-difluoro-4-hydroxyphenyl)aMino]-5,7-diMethyl-8-(3-Methylbutyl)-5,6,7,8-tetrahydropteridin-6-one
- CBNumber:
- CB12460465
- Molecular Formula:
- C19H23F2N5O2
- Molecular Weight:
- 391.42
- MOL File:
- 501437-28-1.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/5/18 11:31:16
| Boiling point | 579.3±60.0 °C(Predicted) |
|---|---|
| Density | 1.297 |
| storage temp. | -20°C |
| solubility | Soluble in DMSO (up to 15 mg/ml) |
| form | Off-white solid. |
| pka | 7.68±0.36(Predicted) |
| color | Off-white |
| 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. |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H315-H319-H227 |
| Precautionary statements | P501-P210-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313-P403+P235 |
| HS Code | 2933599590 |
BI-D1870 Chemical Properties,Uses,Production
Uses
The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility. BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four vertebrate isoforms of RSK, RSK1-4 (IC50s = 31, 24, 18, and 15 nM, respectively). At 100 nM, it also significantly inhibits polo-like kinase 1, Aurora B, maternal embryonic leucine zipper kinase, and mammalian STE20-like kinase 2. BI-D1870 acts at the N-terminal kinase domain, but not the C-terminal domain, of RSK.
Enzyme inhibitor
This cell-permeant, ATP-competitive inhibitor (FW = 391.42 g/mol; CAS 501437-28-1: Solubility = 78 mg/mL DMSO; <1 mg/mL H2O), also known as 2-[ (3,5-difluoro-4-hydroxyphenyl) amino]-7,8-dihydro-5,7-dimethyl-8- (3- methylbutyl) -6 (5H) -pteridinone, targets the p90 Ribosomal protein S6 Kinase a-1, 2, 3, and 4, or RSK1, RSK2, RSK3, and RSK4, with IC50 values of 31 nM, 24 nM, 18 nM, and 15 nM, respectively. RSK isoforms are activated by Extracellular-signal-Regulated Kinases ERK1 and ERK2 in response to growth factors, phorbol esters and other agonists. BI-D1870 shows 10x to 100x selectivity for RSK over MST2, GSK-3β, MARK3, CK1 and Aurora B protein kinases. When tested in vitro, BI-D1870 exhibits IC50 values for inhibits RSK1, RSK2, RSK3 and RSK4 are in the 10–30 nM. Although assumed to be a remarkably specific inhibitor of RSK isoforms, with a >500-fold greater selectivity over nine other AGC kinases, later work assessing the ability of BI-D1870 to protect enzyme active sites from alkylation demonstrated that several other kinases interact with BI-D1870 . Subsequent direct activity assays confirmed that Slk, Lok and Mst1 protein kinases are inhibited by BI-D1870 and that phosphorylation of some of their substrates is blocked by BI-D1870 in living cells. Such results suggest that the specificity of BI-D1870 cannot be taken for certain.
BI-D1870 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32836 | 60 | Inquiry |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | China | 49392 | 58 | Inquiry |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 24099 | 58 | Inquiry |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | China | 3136 | 58 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 | United States | 19973 | 58 | Inquiry |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | China | 8474 | 58 | Inquiry |
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