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MLL1 complex

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) Caspase (1) Epigenetic Reader Domain (1) Histone Methyltransferase (4) Potassium Channel (1) WDR5 (6)
By Research Areas:	Cancer (6) Cardiovascular Disease (2) Inflammation/Immunology (1)

Inhibitors & Agonists

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-175802

HBI-2375 HYBI-084	WDR5 Potassium Channel	Inflammation/Immunology Cancer
HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC₅₀ of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8 ⁺ cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC₅₀ of 17 µM .

HY-P10948A

CS-VIP 8 hydrochloride	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 hydrochloride induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 hydrochloride is promising for research of hematological diseases such as leukemia .

HY-132233A

DDO-2093 dihydrochloride	Histone Methyltransferase	Cancer
DDO-2093 dihydrochloride is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC₅₀=8.6 nM; K_d=11.6 nM) with antitumor activity. DDO-2093 dihydrochloride selectively inhibits the catalytic activity of MLL complex .

HY-132233

DDO-2093	WDR5	Cancer
DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC₅₀=8.6 nM; K_d=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex .

HY-P10948

CS-VIP 8	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .

HY-178752

Z88418521	WDR5	Cancer
Z88418521 is a ligand for the *WDR5-MLL1* complex. Z88418521 may help disrupt the interaction of the *WDR5-MLL1* complex. Z88418521 can be used in cancer research, especially in leukemia .

HY-114162B

VTP50469 mesylate SNDX-50469 mesylate	Epigenetic Reader Domain Apoptosis	Cancer
VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.

HY-183354

HLC40	Histone Methyltransferase WDR5 Apoptosis Caspase	Cancer
HLC40 is a MLL1 histone methyltransferase inhibitor with an IC₅₀ of 0.82 μM by binding to WDR5. HLC40 inhibits proliferation of cancer cells, induces apoptosis and upregulates cleaved caspase-3 levels. HLC40 exhibits antitumor efficacy in a murine AML xenograft model .

Cat. No.	Product Name	Target	Research Area

HY-P10948A

CS-VIP 8 hydrochloride	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 hydrochloride induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 hydrochloride is promising for research of hematological diseases such as leukemia .

HY-P10948

CS-VIP 8	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .

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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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