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SETD8 methyltransferase activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Histone Methyltransferase (3)
By Research Areas:	Cancer (3)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Peptides

Click Chemistry

Targets Recommended: Histone Methyltransferase Amine N-methyltransferase METTL3 COMT ICMT RNA MTase DNA Methyltransferase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-121093

DC-S239	Histone Methyltransferase	Cancer
DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC₅₀ value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity .

HY-P10570

[Nle20] H4 peptide (16−23)	Histone Methyltransferase	Cancer
[Nle20] H4 peptide (16−23) is a peptide with strong inhibitory activity against histone methyltransferase *SETD8* (K_d=0.14 μM), which inhibits *SETD8's methylation of histone H4 by competing with SETD8*'s substrate binding site. [Nle20] H4 peptide (16−23) can be used as a lead compound for anticancer therapy .

HY-181849

MS2928	Histone Methyltransferase	Cancer
MS2928 is a selective *SETD8* inhibitor with an IC₅₀ of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20_me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma .

Cat. No.	Product Name	Target	Research Area

HY-P10570

[Nle20] H4 peptide (16−23)	Histone Methyltransferase	Cancer
[Nle20] H4 peptide (16−23) is a peptide with strong inhibitory activity against histone methyltransferase *SETD8* (K_d=0.14 μM), which inhibits *SETD8's methylation of histone H4 by competing with SETD8*'s substrate binding site. [Nle20] H4 peptide (16−23) can be used as a lead compound for anticancer therapy .

Cat. No.	Product Name		Classification

HY-181849

MS2928		Alkynes
MS2928 is a selective *SETD8* inhibitor with an IC₅₀ of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20_me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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