(R)-DRF053
(R)-DRF053 is a CDK inhibitor. (R)-DRF053 inhibits Cdk5 and promotes the formation of ductal precursor β cells. (R)-DRF053 inhibits Dil-ox-LDL uptake and CD36 gene expression induced by advanced glycation end products (AGEs) in U937 cells.
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- No. CAS: 1056016-06-8
- Fòrmula: C23H27N7O
- Peso molecular:417.51
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
>20 μM
Compound: (R)-DRF053
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Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.093 μM
Compound: (R)-DRF053
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Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.215 μM
Compound: (R)-DRF053
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Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
0.822 μM
Compound: (R)-DRF053
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Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
3.7 μM
Compound: (R)-DRF053
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Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| Sf9 | IC50 |
8 μM
Compound: (R)-DRF053
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Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
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[PMID: 30234987] |
| SH-SY5Y | IC50 |
17.2 μM
Compound: 13a, (R)-DRF053
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Antiproliferative activity against human SH-SY5Y cells assessed as survival after 48 hrs by MTS reduction assay
Antiproliferative activity against human SH-SY5Y cells assessed as survival after 48 hrs by MTS reduction assay
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[PMID: 18698753] |
| SH-SY5Y | IC50 |
17.2 μM
Compound: DRF 53
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Cytotoxicity against human SH-SY5Y cells after 48 hrs by MTS assay
Cytotoxicity against human SH-SY5Y cells after 48 hrs by MTS assay
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[PMID: 23218601] |
Chemical Information
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No. CAS 1056016-06-8
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Peso molecular 417.51
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Fòrmula C23H27N7O
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SMILES
CC(C)N1C2=NC(N[C@@H](CO)CC)=NC(NC3=CC(C4=CC=CC=N4)=CC=C3)=C2N=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Liu KC, et al. Inhibition of Cdk5 Promotes β-Cell Differentiation From Ductal Progenitors. Diabetes. 2018 Jan;67(1):58-70. [Content Brief]
[2]. Yashima H, et al. AGE-RAGE Axis Stimulates Oxidized LDL Uptake into Macrophages through Cyclin-Dependent Kinase 5-CD36 Pathway via Oxidative Stress Generation. Int J Mol Sci. 2020 Dec 4;21(23):9263. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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