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AF9/ENL

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By Targets:	Apoptosis (1) c-Myc (1) Epigenetic Reader Domain (5) Histone Methyltransferase (2) HOXA (1) PROTACs (1)
By Research Areas:	Cancer (6)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145409

SR-0813	Epigenetic Reader Domain	Cancer
SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC₅₀ and EC₅₀ values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC₅₀ and EC₅₀ values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (K_d=3.5 μM) than ENL YEATS (K_d=30 nM). SR-0813 can be used for the research of acute leukemia .

HY-162350

TDI-11055	Epigenetic Reader Domain Apoptosis	Cancer
TDI-11055 is a selective and orally active eleven-nineteen leukemia (ENL) inhibitor, which displaces ENL from chromatin by blocking its YEATS domain interaction with acylated histones. TDI-11055 inhibits ENL and AF9 YEATS domains with IC₅₀ values of 50 nM and 70 nM, respectively, and no activity against GAS41 or YEATS2. TDI-11055 decreases chromatin occupancy of ENL-associated complexes, impairs transcription elongation, suppresses key oncogenic gene expression programs, and induces differentiation. TDI-11055 can be used for the research of acute myeloid leukemia .

HY-178172

AF9/ENL-DOT1L PPI-IN-1	Histone Methyltransferase c-Myc Epigenetic Reader Domain HOXA	Cancer
AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent *AF9/ENL* and histone methyltransferase DOT1L/AF4 protein-protein interactions (PPI) inhibitor. AF9/ENL-DOT1L/AF4 PPI-IN-1 can inhibit the *AF9-DOT1L* (IC₅₀ = 1.5 μM), *AF9-AF4* (IC₅₀ = 1 μM), ENL-AF4 (IC₅₀ = 1.2 μM) interactions. AF9/ENL-DOT1L/AF4 PPI-IN-1 can suppress the expression of Mixed lineage leukemia (MLL) target genes Myc and Meis1 and selectively block the proliferation of MLL-r and several other leukemia cells. AF9/ENL-DOT1L/AF4 PPI-IN-1 exhibits significant antitumor activities in a mouse model of MLL-r leukemia without overt toxicities. AF9/ENL-DOT1L/AF4 PPI-IN-1 can be used for the study of MLL-r leukemia .

HY-146187

Antitumor agent-69	Histone Methyltransferase	Cancer
Antitumor agent-69 (compound 12) is a potent inhibitor of protein-protein interaction between DOT1L and *MLL-AF9/MLL-ENL, with K_is of 9 nM and 109 nM for AF9* and ENL, respectively. Antitumor agent-69 exhibits anticancer cellular activitiy .

HY-183555

MS108	PROTACs Epigenetic Reader Domain	Cancer
MS108 is a selective VHL-based eleven-nineteen leukemia protein (ENL) PROTAC degrader with DC₅₀ of 0.6 nM. MS108 recruits VHL E3 ligase to induce ENL degradation in a VHL- and ubiquitin-proteasome system (UPS)-dependent manner. MS108 degrades the ENL paralog *AF9, which shares a highly conserved YEATS domain with ENL*. MS108 suppresses proliferation of cancer cells .

HY-129224

XS018661	Epigenetic Reader Domain	Cancer
XS018661 is a dual inhibitor of the YEATS domains of ENL and its paralog *AF9* with IC₅₀ values of 1.6 and 3 μM as well as K_d values of 754 nM and 523 nM, respectively .

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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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AF9/ENL

Inhibitors & Agonists