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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
18 Results for "
ENL
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "ENL" in MCE Product Catalog:
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-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 .
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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-169093
CAS No.: 2768610-97-3
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MS41 is a ENL PROTAC degrader with a DC50 of 3.50 nM. MS41 recruits the VHL E3 ubiquitin ligase, triggers ENL degradation via the ubiquitin-proteasome system, and simultaneously induces AF9 degradation. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation complexes, suppresses oncogene expression, and activates differentiation gene expression. MS41 inhibits leukemia cell growth and induces cell cycle arrest and apoptosis. MS41 inhibits leukemia progression in xenograft mouse models. MS41 can be used for research on mixed lineage leukemia-rearranged leukemia and nephroblastoma .
Cat. No.: HY-173631
CAS No.: 3081383-46-9
(S)-dHTC1 is a molecular glue degrader targeting the transcriptional co-activator ENL. (S)-dHTC1 binds the ligase with high affinity only after forming the ENL:dHTC1 complex with an IC50 value of 93 nM. (S)-dHTC1 degrades ENL in MV4;11 cells with a DC50 value of 26 nM. (S)-dHTC1 can be used for acute myeloid leukemia study .
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-169094
CAS No.: 2768514-05-0
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PFI-6-COOH (Compound 18) is an eleven-nineteen leukemia (ENL) ligand, and can be used for synthesis of MS41 (HY-169093), an ENL PROTAC degrader .
Cat. No.: HY-169937
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(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .
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-152469
CAS No.: 2894121-68-5
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Eleven-Nineteen-Leukemia Protein IN-1 is an inhibitor of ENL YEATS domain with an IC50 value of 14.5 nM. Eleven-Nineteen-Leukemia Protein IN-1 interacts with ENL protein and enhances the thermal stability of ENL protein in vitro .
Cat. No.: HY-152471
CAS No.: 2894121-83-4
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Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro .
Cat. No.: HY-RS08493
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MLLT1 Human Pre-designed siRNA Set A contains three designed siRNAs for MLLT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-152470
CAS No.: 2894121-78-7
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Eleven-Nineteen-Leukemia Protein IN-2 (compound 23) is an Eleven-Nineteen-Leukemia Protein (ENL) inhibitor with an IC50 value of 10.7 nM. Eleven-Nineteen-Leukemia Protein IN-2 can be used for the research of leukemia .
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-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 .
Cat. No.: HY-183825
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Eleven-Nineteen-Leukemia Protein IN-4 is a ENL YEATS domain inhibitor with an IC50 of 62.0 nM and a Kd of 100.4 nM. Eleven-Nineteen-Leukemia Protein IN-4 downregulates MYC expression and inhibits cancer cell growth; it exerts a synergistic effect with the bromodomain inhibitor JQ-1 (HY-13030). Eleven-Nineteen-Leukemia Protein IN-4 can be used in the research of acute myeloid leukemia .
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-181976
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dHTC3 is a selective BRD4 molecular glue degrader. dHTC3 specifically recruits the first bromodomain of BRD4 to the E3 ubiquitin ligase complex (SCF FBXO3), thereby triggering the ubiquitination and degradation of BRD4 .
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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
