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MLL-rearranged leukemia

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (8) Caspase (1) Drug Isomer (1) Epigenetic Reader Domain (9) FLT3 (2) Histone Methyltransferase (8) Ligands for Target Protein for PROTAC (1) Mitochondrial Metabolism (1) Potassium Channel (1) PROTACs (4) WDR5 (2)
By Research Areas:	Cancer (19) Cardiovascular Disease (2) Inflammation/Immunology (3)

Targets Recommended: BMI1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-136175

Revumenib Maximum Cited Publications 15 Publications Verification SNDX-5613	Epigenetic Reader Domain	Cancer
Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding K_i of 0.149 nM and a cell based IC₅₀ of 10-20 nM. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) .

HY-15227

EPZ004777 5+ Cited Publications	Histone Methyltransferase Apoptosis	Inflammation/Immunology Cancer
EPZ004777 is an effective and selective DOT1L inhibitor, with IC₅₀ being 0.4 nM. EPZ004777 reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 can be used for the study of leukemia .

HY-15222

Menin-MLL inhibitor MI-2 4 Publications Verification	Epigenetic Reader Domain Apoptosis	Cancer
Menin-MLL inhibitor MI-2 is a competitive and selective Menin-MLL interaction inhibitor with an IC₅₀ value of 446 nM and a K_i value of 158 nM. Menin-MLL inhibitor MI-2 downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL) .

HY-162250

MS8847	PROTACs Histone Methyltransferase	Cancer
MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC₅₀=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer .

HY-156794

Enzomenib DSP-5336	Epigenetic Reader Domain FLT3	Cancer
Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC₅₀=1.4 nM, K_d=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations .

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-15227A

EPZ004777 hydrochloride 5+ Cited Publications	Histone Methyltransferase Apoptosis	Inflammation/Immunology Cancer
EPZ004777 hydrochloride is an effective and selective DOT1L inhibitor, with IC₅₀ being 0.4 nM. EPZ004777 hydrochloride reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 hydrochloride selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 hydrochloride can be used for the study of leukemia .

HY-114410

CCI-006	Mitochondrial Metabolism	Cancer
CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells .

HY-15222A

Menin-MLL inhibitor MI-2 dihydrochloride	Epigenetic Reader Domain Apoptosis	Cancer
Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective Menin-MLL interaction inhibitor with an IC₅₀ value of 446 nM and a K_i value of 158 nM. Menin-MLL inhibitor MI-2 dihydrochloride downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL) .

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-122698

CCI-007	Apoptosis	Cancer
CCI-007 is a small molecule with cytotoxic activity against infant leukemia with MLL rearrangements, with IC₅₀ values of 2.5-6.2 μM in sensitive cells .

HY-181834

PROTAC MLLT1 Degrader-1	PROTACs Epigenetic Reader Domain	Cancer
PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML) .

HY-181787

DOT1L705	PROTACs Histone Methyltransferase	Cardiovascular Disease
DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia .

HY-181790

DOT1L ligand-2	Ligands for Target Protein for PROTAC Histone Methyltransferase	Cancer
DOT1L ligand-2 (Compound 52) is a DOT1L ligand. DOT1L ligand-2 acts as a Ligand for Target Protein for PROTAC, which is used to develop and design degraders of PROTAC DOT1L, such as DOT1L808 (HY-181789). DOT1L ligand-2 is applicable to research related to MLL-rearranged leukemia .

HY-181690

Menin-MLL-IN-37	Epigenetic Reader Domain	Cancer
Menin-MLL-IN-37 is an orally active Menin-MLL protein complex inhibitor with an IC₅₀of 820.50 nM. Menin-MLL-IN-37 disrupts the interaction between menin and MLL proteins. Menin-MLL-IN-37 induces differentiation of acute myeloid leukemia cells and selectively inhibits the proliferation of MLL-rearranged and DNMT3A/NPM1-mutant leukemia cells. Menin-MLL-IN-37 can be used for the research of acute myeloid leukemia (AML) .

HY-136175B

cis-Revumenib cis-SNDX-5613	Epigenetic Reader Domain	Cancer
cis-Revumenib (cis-SNDX-5613) is an isomer of Revumenib (HY-136175). Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding K_i of 0.149 nM and a cell based IC₅₀ of 10-20 nM. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) .

HY-115619

EPZ004777 formate	Histone Methyltransferase Apoptosis	Cancer
EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC₅₀ being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia .

HY-156794A

Enzomenib enantiomer DSP-5336 enantiomer	Drug Isomer FLT3 Epigenetic Reader Domain	Cardiovascular Disease Cancer
Enzomenib enantiomer (DSP-5336 enantiomer) is an enantiomer of Enzomenib (HY-156794). Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC₅₀=1.4 nM, K_d=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations .

HY-181789

DOT1L808	PROTACs Histone Methyltransferase	Cancer
DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC₅₀ value of 5 nM. DOT1L808 can promote the ubiquitination and degradation of DOT1L. DOT1L808 exhibits antitumor activity in an orthotopic leukemia model .

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 .

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MLL-rearranged leukemia

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