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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
14 Results for "
AF9
" in MedChemExpress (MCE) Product Catalog:
Products (14)
14 Results for "AF9" in MCE Product Catalog:
2
2 Cited Publications
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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 .
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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 .
Cat. No.: HY-162350
CAS No.: 3057216-63-1
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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 .
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SR-1114 is a ENL PROTAC degrader, with DC50 values of 150 nM, 311 nM and 1.65 μM in MV4;11, MOLM-13 and OCI/AML-2 cells, respectively. SR-1114 has an IC50 of 155 nM against the human CRL4CRBN complex. SR-1114 can be used in research related to acute leukemia and acute myeloid leukemia .
Cat. No.: HY-178172
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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 .
Cat. No.: HY-169093
CAS No.: 2768610-97-3
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MS41 is a selective ENL PROTAC degrader with DC50 values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat) and 26.58 nM (KASUMI1), respectively. MS41 recruits the VHL E3 ubiquitin ligase, induces ubiquitination and degradation of ENL (including mutant ENL carrying mutations in the YEATS domain), and reduces the chromatin occupancy of ENL-associated transcription elongation complexes. MS41 induces G1 phase cell cycle arrest and Apoptosis. MS41 inhibits leukemia progression in xenograft models. MS41 can be used in research related to mixed lineage leukemia-rearranged leukemia and Wilms tumor .
Cat. No.: HY-146187
CAS No.: 2417651-42-2
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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 .
Cat. No.: HY-19541A
CAS No.: 2147701-33-3
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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 .
Cat. No.: HY-146724
CAS No.: 2580940-76-5
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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 .
Cat. No.: HY-129224
CAS No.: 878415-59-9
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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 .
Cat. No.: HY-183555
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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 .
Cat. No.: HY-RS08496
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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.
Cat. No.: HY-182019
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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 .
Cat. No.: HY-184342
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SYC-2863 is a CRBN-recruiting PROTAC degrader that selectively degrades ENL (MLLT1), with an ENL DC50 of 45 nM in MV4;11 cells. SYC-2863 inhibits the proliferation of MLL-rearranged leukemia and multiple myeloma cells. After degrading intracellular ENL, SYC-2863 dose-dependently downregulates the transcription levels of MYC and its downstream target genes, blocking the MYC-mediated malignant proliferation pathway. SYC-2863 can be used in studies related to MLL-rearranged leukemia and multiple myeloma .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
