CDK9-Cyclin T1 PPI-IN-1

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CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC₅₀: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model.

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CDK9-Cyclin T1 PPI-IN-1 Chemical Structure

CAS No. : 2995336-58-6

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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
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.441 μM Compound: B19	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
A549	IC₅₀	2.305 μM Compound: B19	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
BT-549	IC₅₀	0.147 μM Compound: B19	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
HEK-293T	IC₅₀	> 0.8 μM Compound: 6; B19	Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 38564299]
HK-2	IC₅₀	0.481 μM Compound: B19	Cytotoxicity against HK-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against HK-2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
HeLa	IC₅₀	0.158 μM Compound: B19	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
HepG2	IC₅₀	0.392 μM Compound: B19	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
Hs-578T	IC₅₀	0.131 μM Compound: B19	Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human Hs-578T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
L02	IC₅₀	0.756 μM Compound: B19	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
L02	IC₅₀	> 0.8 μM Compound: 6; B19	Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 38564299]
MCF-10A	IC₅₀	0.498 μM Compound: B19	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
MDA-MB-231	IC₅₀	0.044 μM Compound: B19	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
MDA-MB-231	IC₅₀	1.61 μM Compound: B19	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay	[PMID: 37837671]
MDA-MB-231	IC₅₀	201 nM Compound: B19	Antiproliferative activity against human MDA-MB-231 cells transfected with shCDK9 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells transfected with shCDK9 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]
MRC5	IC₅₀	0.335 μM Compound: B19	Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37837671]

Molecular Weight

404.46

Formula

C₂₃H₂₄N₄O₃

CAS No.

2995336-58-6

SMILES

COC1=CC=C(C=C1)C(NC2=CC(C3=CC(N4CCC(CC4)O)=NC=C3)=CC=N2)=O

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]. Gao G, et al. Design, synthesis, and biological evaluation of novel 4,4'-bipyridine derivatives acting as CDK9-Cyclin T1 protein-protein interaction inhibitors against triple-negative breast cancer. Eur J Med Chem. 2023 Oct 6;261:115858. [Content Brief]