DNMT/HDAC-IN-1

Cat. No.: HY-158075: FAQs
Data Sheet Handling Instructions

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DNMT/HDAC-IN-1 (Compund 15a) is a dual DNMT and HDAC inhibitor with IC₅₀ values for HDAC1 and HDAC6 are 56.84 nM and 17.39 nM respectively. DNMT/HDAC-IN-1 can induce apoptosis and be used in tumor research.

For research use only. We do not sell to patients.

DNMT/HDAC-IN-1 Chemical Structure

CAS No. : 2095619-17-1

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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DNA Methyltransferase DNMT1 DNMT3 MGMT

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

HDAC1

56.84 nM (IC₅₀)

HDAC6

17.39 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
K562	IC₅₀	2.85 μM Compound: 15a	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay Antiproliferative activity against human K562 cells after 72 hrs by MTT assay	[PMID: 28419930]
U-937	IC₅₀	1.06 μM Compound: 15a	Antiproliferative activity against human U937 cells after 72 hrs by MTT assay Antiproliferative activity against human U937 cells after 72 hrs by MTT assay	[PMID: 28419930]

In Vitro

DNMT/HDAC-IN-1 significantly suppress K562 and U937 proliferation with IC₅₀ values of 2.85 and 1.06 mM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	U937 cells
Concentration:	0, 1, 2.5, 5 μM
Incubation Time:	12 h
Result:	induced histone H3K9 and histone H4K8 acetylation and increased P16 expression.

Apoptosis Analysis^[1]

Cell Line:	U937 cells
Concentration:	2.5, 5, 10 μM
Incubation Time:	36 h
Result:	induced apoptosis in U937 cells.

In Vivo

Animal Model:	female BALB/c wild-type mice^[2]
Dosage:	50 mg/kg
Administration:	I.v.; daily; 21 days
Result:	inhibited tumor growth.

Molecular Weight

412.79

Formula

C₁₉H₁₆ClF₃N₂O₃

CAS No.

2095619-17-1

SMILES

O=C(NO)/C=C/C1=CC=C(C=C1)CCNC(C2=C(C=CC(C(F)(F)F)=C2)Cl)=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]. Yuan Z, et al. Design, synthesis and anticancer potential of NSC-319745 hydroxamic acid derivatives as DNMT and HDAC inhibitors. Eur J Med Chem. 2017 Jul 7;134:281-292. [Content Brief]

[2]. Huang W, et al. Dual inhibitors of DNMT and HDAC induce viral mimicry to induce antitumour immunity in breast cancer. Cell Death Discov. 2024 Mar 15;10(1):143. [Content Brief]

DNMT/HDAC-IN-1 Related Classifications

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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

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

DNMT/HDAC-IN-12095619-17-1HDACDNA MethyltransferaseHistone deacetylasesDNMTsDNA MTasesEpigenetic targetsMulti-targetAntitumor bioactivityDNMTInhibitorinhibitorinhibit

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