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Results for "

AF9

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

1

Oligonucleotides

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 (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia .
    SR-0813
  • HY-112804
    SGC-iMLLT
    2 Publications Verification

    		 Epigenetic Reader Domain Cancer
    SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with Kds of 0.129 and 0.077 μM, respectively .
    SGC-iMLLT
  • 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 .
    TDI-11055
  • 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 .
    AF9/ENL-DOT1L PPI-IN-1
  • 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 Kis of 9 nM and 109 nM for AF9 and ENL, respectively. Antitumor agent-69 exhibits anticancer cellular activitiy .
    Antitumor agent-69
  • HY-19541A
    I-CBP112 hydrochloride

    		Epigenetic Reader Domain Cancer
    I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin .
    I-CBP112 hydrochloride
  • HY-146724
    Dot1L-IN-7

    		Histone Methyltransferase Cancer
    Dot1L-IN-7 (compound 25) is a potent and selective disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 1.0 μM. Dot1L-IN-7 selectively killed Mixed Lineage Leukemia (MLL)-AF9 without showing any effect on the growth of E2A-HLF cells .
    Dot1L-IN-7
  • 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 Kd values of 754 nM and 523 nM, respectively .
    XS018661
  • 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 .
    MS108
  • HY-RS08496
    MLLT3 Human Pre-designed siRNA Set A

    		Small Interfering RNA (siRNA) Others

    MLLT3 Human Pre-designed siRNA Set A contains three designed siRNAs for MLLT3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    MLLT3 Human Pre-designed siRNA Set A
    MLLT3 Human Pre-designed siRNA Set A
  • HY-182019
    HDAC11-IN-5

    		HDAC SHMT Apoptosis Reactive Oxygen Species (ROS) Ferroptosis Cancer
    HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC50 of 0.021 μM. HDAC11-IN-5 increases fatty acylation levels of substrate SHMT2 in AML cells. HDAC11-IN-5 induces apoptosis, G1 phase cell cycle arrest, ferroptosis, ROS production and terminal myeloid differentiation in AML cells. HDAC11-IN-5 demonstrates anti-tumor potency in an MLL-AF9-induced mouse AML model. HDAC11-IN-5 can be used for the research of cancer, such as acute myeloid leukemia .
    HDAC11-IN-5

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