(R)-DRF053

Cat. No.: HY-10380: Data Sheet Handling Instructions
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(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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(R)-DRF053 Chemical Structure

CAS No. : 1056016-06-8

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Other In-stock Forms of (R)-DRF053:

(R)-DRF053 dihydrochloride

Other Forms of (R)-DRF053:

(R)-DRF053 dihydrochloride In-stock

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•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	>20 μM Compound: (R)-DRF053	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	[PMID: 30234987]
Sf9	IC₅₀	0.093 μM Compound: (R)-DRF053	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	[PMID: 30234987]
Sf9	IC₅₀	0.215 μM Compound: (R)-DRF053	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	[PMID: 30234987]
Sf9	IC₅₀	0.822 μM Compound: (R)-DRF053	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	[PMID: 30234987]
Sf9	IC₅₀	3.7 μM Compound: (R)-DRF053	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	[PMID: 30234987]
Sf9	IC₅₀	8 μM Compound: (R)-DRF053	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	[PMID: 30234987]
SH-SY5Y	IC₅₀	17.2 μM Compound: 13a, (R)-DRF053	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	[PMID: 18698753]
SH-SY5Y	IC₅₀	17.2 μM Compound: DRF 53	Cytotoxicity against human SH-SY5Y cells after 48 hrs by MTS assay Cytotoxicity against human SH-SY5Y cells after 48 hrs by MTS assay	[PMID: 23218601]

Molecular Weight

417.51

Formula

C₂₃H₂₇N₇O

CAS No.

1056016-06-8

SMILES

CC(C)N1C2=NC(N[C@@H](CO)CC)=NC(NC3=CC(C4=CC=CC=N4)=CC=C3)=C2N=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

(R)-DRF053 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(R)-DRF0531056016-06-8CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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