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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
26 Results for "
EHMT
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "EHMT" in MCE Product Catalog:
12
12 Publications Verification
UNC0638, a chemical probe, selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 inhibits TNBC cell invasion and migration in vitro. UNC0638 is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets .
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7 Cited Publications
Forschungsgebiete:
A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
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EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer .
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EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer .
Art. -Nr.: HY-161759
CAS. Nr.: 3107476-89-8
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MS152 is an orally active, blood-brain barrier penetrant inhibitor of EHMT2/G9a and EHMT1/GLP, with IC50s of 76 nM and 126 nM, repsectively. MS152 reduces H3K9me2 levels and reactivates maternally silenced Prader-Willi syndrome (PWS) genes. MS152 significantly improves perinatal lethality and growth retardation in mouse models, and is applicable to research related to Prader-Willi syndrome .
Art. -Nr.: HY-44062
CAS. Nr.: 1350752-07-6
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G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer .
Art. -Nr.: HY-176036
CAS. Nr.: 3070323-06-4
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MS1262 is a blood-brain barrier-permeable, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), with an IC50 of 19 nM and a Kd of 74 nM against G9a, and an IC50 of 6 nM and a Kd of 19 nM against GLP. MS1262 reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 restores hippocampal long-term potentiation (LTP) and miniature excitatory postsynaptic current (sEPSC) frequency, ameliorates spatial memory deficits, and reverses anxiety-like and depression-like behaviors in AD model mice. MS1262 reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 reduces the risk of thrombus rupture. MS1262 can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer .
Art. -Nr.: HY-RS04227
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EHMT1 Human Pre-designed siRNA Set A contains three designed siRNAs for EHMT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Art. -Nr.: HY-RS04228
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Ehmt1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ehmt1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Art. -Nr.: HY-RS04229
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EHMT1 Rat Pre-designed siRNA Set A contains three designed siRNAs for EHMT1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Art. -Nr.: HY-RS04230
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EHMT2 Human Pre-designed siRNA Set A contains three designed siRNAs for EHMT2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Art. -Nr.: HY-RS04231
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Ehmt2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ehmt2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Art. -Nr.: HY-RS04232
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Ehmt2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Ehmt2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Art. -Nr.: HY-133031
CAS. Nr.: 442150-41-6
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CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294 .
Art. -Nr.: HY-110093
CAS. Nr.: 1255517-77-1
UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 hydrate inhibits TNBC cell invasion and migration in vitro. UNC0638 hydrate is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 hydrate has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets .
Art. -Nr.: HY-111778R
CAS. Nr.: 2230849-55-3
Forschungsgebiete:
EHMT2-IN-1 (Standard) is the analytical standard of EHMT2-IN-1 (HY-111778). This product is intended for research and analytical applications. EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer .
Art. -Nr.: HY-133031A
CAS. Nr.: 474084-56-5
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CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
Art. -Nr.: HY-184500
CAS. Nr.: 2923223-81-6
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TNG917 is a potent, selective EHMT1/2 inhibitor with oral activity. TNG917 reduces H3K9me2-mediated transcriptional repression, restores interferon-stimulated gene expression, promotes the secretion of T-cell chemokines such as CXCL10, and converts immunologically cold tumors into T-cell inflamed tumors. TNG917 is applicable to studies on immunologically cold tumors, colorectal cancer, anti-tumor immunity, interferon signaling pathways and epigenetic immune escape .
Art. -Nr.: HY-183058
CAS. Nr.: 2140164-84-5
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EZM8266 is an orally active and selective G9a (EHMT2) histone methyltransferase inhibitor with a human EHMT2 IC50 of 1 pM. EZM8266 reduces repressive H3K9me2 marks at immune-stimulatory gene and endogenous retroviral element promoters. EZM8266 reduces colony formation, migration, and invasion of cancer cells. EZM8266 enhances IFN-γ response, increases MHC class I expression, and enhances CXCL10-mediated T cell recruitment in cancer cells. EZM8266 can be used for the research of hepatocellular carcinoma .
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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
