CDK9/EZH2-IN-1

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CDK9/EZH2-IN-1 is a CDK9/EZH2 dual-target inhibitor (IC₅₀: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC₅₀ values are 136.3, 171.3 and 315.7 nM, respectively).

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CDK9/EZH2-IN-1 Chemical Structure

CAS No. : 3081246-18-3

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
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Description

IC₅₀ & Target^[1]

CDK9

83.9 nM (IC₅₀)

EZH2

108.6 nM (IC₅₀)

Molecular Weight

906.17

Formula

C₄₇H₅₉N₁₁O₄S₂

CAS No.

3081246-18-3

SMILES

CC1=CC(C)=C(C(N1)=O)CNC(C2=CC(C3=CC=C(N=C3)N4CCN(CC4)CCN5CCC(CC5)C(NC6=NC=C(S6)SCC7=NC=C(O7)C(C)(C)C)=O)=CC8=C2C=NN8C(C)C)=O

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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]. Tian L, et al. Design and synthesis of CDK9/EZH2 dual-target inhibitors to achieve synergistic antitumor effects. Eur J Med Chem. 2025 May 17;294:117773. [Content Brief]

CDK9/EZH2-IN-1 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
C1		V1		C2		V2

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:

CDK9/EZH2-IN-13081246-18-3CDKHistone MethyltransferaseCyclin dependent kinaseAnticancerMKN45MDA-MB-453SW620B-cell Lymphoma (DLBCL) cell linesInhibitorinhibitorinhibit

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