Aloisine A

Modify Date: 2024-01-31 13:29:32

Aloisine A structure	Common Name	Aloisine A
	CAS Number	496864-16-5	Molecular Weight	267.32600
	Density	1.227g/cm3	Boiling Point	N/A
	Molecular Formula	C₁₆H₁₇N₃O	Melting Point	281-283ºC
	MSDS	N/A	Flash Point	N/A

Use of Aloisine A

Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 µM) and GSK-3β (IC50=1.5 µM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research[1][2].

Name	4-(7-butyl-1,5-dihydropyrrolo[2,3-b]pyrazin-6-ylidene)cyclohexa-2,5-dien-1-one
Synonym	More Synonyms

Description	Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 µM) and GSK-3β (IC50=1.5 µM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research[1][2].
Related Catalog	Signaling Pathways >> Stem Cell/Wnt >> GSK-3 Signaling Pathways >> Membrane Transporter/Ion Channel >> CFTR Research Areas >> Cancer Research Areas >> Inflammation/Immunology Signaling Pathways >> Cell Cycle/DNA Damage >> CDK Signaling Pathways >> MAPK/ERK Pathway >> ERK Signaling Pathways >> MAPK/ERK Pathway >> JNK Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3 Signaling Pathways >> Stem Cell/Wnt >> ERK
Target	CDK1/cyclinB:0.15 μM (IC50) CDK2/cyclinA:0.12 μM (IC50) CDK2/cyclinE:0.4 μM (IC50) CDK5/p35:0.16 μM (IC50) GSK-3β:0.5 μM (IC50) GSK-3α:1.5 μM (IC50) JNK:3-10 μM (IC50) ERK1:18 μM (IC50) ERK2:22 μM (IC50)
In Vitro	Aloisine A ininhibits erk1 (IC50=18 µM), erk2 (IC50=22 µM), c-Jun N-terminal kinase (JNK; IC50~3-10 µM). Aloisine A has no effect on protein kinase C α, β1, β2, γ, δ, ε, η, ξ (all IC50>100 µM)[1]. Aloisine A (0.1, 1, 10, 100 µM) completely blocks the proliferation of dividing NT2 cells (IC50=7 μM) and differentiated postmitotic neurons (hNT; IC50=10.5 μM), and very few cells actually die[1]. Aloisine A acts as a submicromolar activator of wild-type (WT)-CFTR [human airway epithelial Calu-3 and WT-CFTR-Chinese hamster ovary (CHO) cells], G551D-CFTR (G551D-CFTR-CHO cells), and F508del-CFTR (in temperature-corrected human airway epithelial F508del/F508del CF15 cells)[2].
References	[1]. Yvette Mettey, et al. Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003 Jan 16;46(2):222-36. [2]. Sabrina Noel, et al. Discovery of pyrrolo[2,3-b]pyrazines derivatives as submicromolar affinity activators of wild type, G551D, and F508del cystic fibrosis transmembrane conductance regulator chloride channels. J Pharmacol Exp Ther. 2006 Oct;319(1):349-59.

Density	1.227g/cm3
Melting Point	281-283ºC
Molecular Formula	C₁₆H₁₇N₃O
Molecular Weight	267.32600
Exact Mass	267.13700
PSA	61.80000
LogP	3.67310
Index of Refraction	1.655

HS Code	2933990090

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

1ung

RP107

Aloisine A RP107

ALOISINE A

ALH

4-(7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)phenol

DC Chemicals Limited
China
Product Name: Aloisine A
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 4-(7-BUTYL-5H-PYRROLO[2,3-B]PYRAZIN-6-YL)PHENOL
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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