BI-D1870

ChemicalBook > CAS DataBase List > BI-D1870

Product Name: 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
Formula Weight: 391.42
MOL File: 501437-28-1.mol

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BI-D1870 Property

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.

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Safety

HS Code: 2933599590

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H227Combustible liquid

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P370+P378In case of fire: Use … for extinction.

P403+P235Store in a well-ventilated place. Keep cool.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Alfa Aesar

Product number: J67102
Product name: BI-D1870, 98%
Packaging: 1mg
Price: $77.8
Updated: 2021/12/16

Alfa Aesar

Product number: J67102
Product name: BI-D1870, 98%
Packaging: 5mg
Price: $264
Updated: 2021/12/16

Cayman Chemical

Product number: 15264
Product name: BI-D1870
Purity: ≥95%
Packaging: 1mg
Price: $56
Updated: 2024/03/01

Cayman Chemical

Product number: 15264
Product name: BI-D1870
Purity: ≥95%
Packaging: 5mg
Price: $201
Updated: 2024/03/01

Cayman Chemical

Product number: 15264
Product name: BI-D1870
Purity: ≥95%
Packaging: 10mg
Price: $322
Updated: 2024/03/01

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BI-D1870 Chemical Properties,Usage,Production

Description

BI-D1870 (501437-28-1) is an inhibitor of p90 ribosomal S6 kinase (RSK; IC50’s = RSK1, 31 nM; RSK2, 24 nM; RSK3, 18 nM; RSK4, 15 nM) with selectivity over other AGC kinases.1?It protected mice from experimental autoimmune encephalomyelitis suggesting a new strategy to treat multiple sclerosis.2?BI-D1870 has also been found to alter mTORC1 signaling in an RSK-independent manner.3?BI-D1870 induced apoptosis in oral squamous cell carcinoma cells4, suppressed growth and induced apoptosis in pediatric medulloblastoma cell lines as well as sensitizing these lines to Sonic hedgehog agents5, and blocked cell proliferation and protein synthesis in dual BRAF and MEK inhibitor-resistant melanoma6.

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.

target

RSK4

References

1) Gopal?et al. (2007),?BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo; Biochem. J.?401 (Pt 1)?29 2) Takda?et al.?(2016),?The ribosomal S6 kinase inhibitor BI-D1870 ameliorated experimental autoimmune encephalomyelitis in mice;?Immunobiology?221?188 3) Roffe?et al.?(2015),?Two widely used RSK inhibitors, BI-D1870 and SL0101, alter mTORC1 signaling in a RSK-independent manner; Cell Signal.?27?1630 4) Chiu?et al.?(2014),?Antitumor effects of BI-D1870 on human oral squamous cell carcinoma; Cancer Chemother. Pharmacol.?73?237 5) Pambid?et al. (2014),?Overcoming resistance to Sonic hedgehog inhibition by targeting p90 ribosomal S6 kinase in pediatric medulloblastoma; Pediatr. Blood Cancer?61?107 6) Theodosakis?et al.?(2017),?p90RSK Blockade Inhibits Dual BRAF and MEK Inhibitor-Resistant Melanoma by Targeting Protein Synthesis; J. Invest. Dermatol.?137?2187

BI-D1870 Preparation Products And Raw materials

Raw materials

Preparation Products

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501437-28-1, BI-D1870Related Search:

Brefeldin A Ko 143 ZM 336372 CL 82198 HYDROCHLORIDE MK-2206 2HCl JNJ-7706621 PF-4708671 SCH772984 Rapamycin AT9283

2-(3,5-Difluoro-4-hydroxyphenylamino)-5,7-dimethyl-8-(3-methylbutyl)-7,8-dihydro-5H-pteridin-6-one

CS-606

BID1870;BI-D 1870

BI-D1870

2-[(3,5-difluoro-4-hydroxyphenyl)aMino]-5,7-diMethyl-8-(3-Methylbutyl)-5,6,7,8-tetrahydropteridin-6-one

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]-7,8-DIHYDRO-5,7-DIMETHYL-8-(3-METHYLBUTYL)-6(5H)-PTERIDINONE

BI-D1870 USP/EP/BP

BI-D1870 RSK Inhibitor II

501437-28-1

C19H24FN5O2

C19H23F2N5O2

Inhibitors