2866408-21-9
2866408-21-9
Chemical Structure
MS8511
- CAS No.: 2866408-21-9
- Formula:C28H41N5O3
- Molecular Weight:495.66
IUPAC Name: N-(4-((1-isopropylpiperidin-4-yl)amino)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinolin-2-yl)acrylamide
InChIKey: FNRUPVONTWZCGL-UHFFFAOYSA-N
SMILES: COC1=CC(C(C=C1OCCCN2CCCC2)=NC(NC(C=C)=O)=C3)=C3NC4CCN(CC4)C(C)C
Biological Activity: MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS)[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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MS8511 | MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS). | |||||||||||||||||||||
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UNC0638 hydrate | 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. | |||||||||||||||||||||
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UNC0646 | 99.38% | UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM. | ||||||||||||||||||||
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UNC0642 | 99.42% | UNC0642, a chemical probe, is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC50 of <2.5 nM for G9a. | ||||||||||||||||||||
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MS8511 hydrochloride | 98.07% | MS8511 (hydrochloride) is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 (hydrochloride) reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 (hydrochloride) can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS). | ||||||||||||||||||||
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UNC0638 | 99.84% | 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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Antitumor agent-101 | Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model. | |||||||||||||||||||||
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W4275 | 98.93% | W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research. | ||||||||||||||||||||
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UNC0737 | 99.70% | UNC0737 is an orthosteric choline kinase inhibitor. UNC0737 is also a poor inhibitor of G9a (IC50 = 5000 nM) and GLP (IC50 > 10000 nM) in the SAHH-coupled assays. | ||||||||||||||||||||
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MS1262 | 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. | |||||||||||||||||||||
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G9a-IN-1 | 98.12% | 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. | ||||||||||||||||||||
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