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HomeProduct name listRP107

RP107

Synonym(s):Aloisine A - CAS 496864-16-5 - Calbiochem;RP107, 7- n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine

RP107 Structural

What is RP107?

Chemical properties

Yellow solid

The Uses of RP107

A cell-permeable pyrrolo-pyrazine compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin dependent kinases (Cdks: IC50 =150nM, 120 nM, 400 nM and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25,

What are the applications of Application

Aloisine A is an inhibitor of CDK1, CDK2, CDK5, GSK-3 alpha, and JNK

Definition

ChEBI: 4-(7-butyl-1,5-dihydropyrrolo[2,3-b]pyrazin-6-ylidene)-1-cyclohexa-2,5-dienone is a member of quinomethanes.

General Description

A cell-permeable pyrrolo-pyrazine compound that exerts anti-proliferative effects. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks; IC50 = 150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively), glycogen synthase kinase-3 (GSK-3; IC50 = 500 nM and 1.5 μM for GSK-3α, GSK-3β, respectively), and c-Jun N-terminal kinase (JNK; IC50 = ~ 3 - 10 μM). It inhibits several other enzymes (CK1, CK2, MAPKK, PKA, PKG, PKCs, and c-raf) poorly (IC50 ≥ 100 μM). Shown to arrest cells in both G1 and G2 phases (IC50 = 7 μM and 10.5 μM for undifferentiated human teratocarcinoma cells NT2 and differentiated postmitotic neurons hNT, respectively). Shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 μM Forskolin (Cat. No. 344270) with high affinity (EC50 = 150 nM, 140 nM and 111 nM, respectively).

Biochem/physiol Actions

EC50 = 150 nM, 140 nM and 111 nM, in stimulating CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 μM Forskolin, respectively

Properties of RP107

Melting point: 281-283°C
Density  1.227
storage temp.  Keep in dark place,Sealed in dry,2-8°C
solubility  DMSO (Slightly), Methanol (Slightly)
pka 9.67±0.15(Predicted)
form  Yellow solid
color  Light Orangish Yellow

Safety information for RP107

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for RP107

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