496864-16-5
496864-16-5 structure
- Name: Aloisine A
- Chemical Name: 4-(7-butyl-1,5-dihydropyrrolo[2,3-b]pyrazin-6-ylidene)cyclohexa-2,5-dien-1-one
- CAS Number: 496864-16-5
- Molecular Formula: C16H17N3O
- Molecular Weight: 267.32600
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2018-12-05 12:28:30
- Modify Date: 2024-01-31 13:29:32
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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 |
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| Synonyms |
1ung
RP107 Aloisine A RP107 ALOISINE A ALH 4-(7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)phenol |
| 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]. |
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| Related Catalog | |
| 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 |
| 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 |
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| HS Code | 2933990090 |
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| 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% |