MAK683 - 99%, high purity , CAS No.1951408-58-4, Allosteric modulator of embryonic ectoderm development

Item Number
M414309
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M414309-1mg
1mg
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$29.90
M414309-5mg
5mg
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M414309-10mg
10mg
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M414309-25mg
25mg
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M414309-50mg
50mg
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Histone Methyltransferase Inhibitors

Basic Description

SynonymsA16922 | 1951408-58-4 | D93894 | BDBM291687 | EED inhibitor-1 | UNII-4K446Z8N51 | 4K446Z8N51 | N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine | AC-30344 | MAK683 | MAK-683 | example 2 [W
Specifications & PurityMoligand™, ≥97%
Biochemical and Physiological MechanismsMAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeALLOSTERIC MODULATOR
Mechanism of actionAllosteric modulator of embryonic ectoderm development
Product Description

Information

MAK683 MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED) . MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively.


Targets

EED (ELISA assay); EED (EED Alphascreen binding assay); EED (LC-MS assay) 26 nM; 59 nM; 89 nM


In vitro

MAK-683 binds to EED and disrupts the PRC2 complex. Cell viability is not significantly affected and the levels of H3K27me3 are decreased. A significant increase in the percentage of mature PCs after MAK-683 treatment in association with a higher CD38 expression is also identified.


Cell Research(from reference)

Cell lines:MBCs 

Concentrations:2\u2009µM 

Incubation Time:4 days, 3 days 

Associated Targets(Human)

EED Tchem Polycomb protein EED (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC18A2 Tclin Synaptic vesicular amine transporter (118 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A5 Tclin Cytochrome P450 3A5 (525 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EED Tchem Polycomb protein EED (645 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Pde4d Phosphodiesterase 4D (4 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NIH3T3 (5395 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CT26 (928 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine
INCHI InChI=1S/C20H17FN6O/c1-12-13(3-2-7-22-12)16-10-24-20(27-11-25-26-19(16)27)23-9-15-14-6-8-28-18(14)5-4-17(15)21/h2-5,7,10-11H,6,8-9H2,1H3,(H,23,24)
InChi Key XLIBABIFOBYHSV-UHFFFAOYSA-N
Canonical SMILES CC1=C(C=CC=N1)C2=CN=C(N3C2=NN=C3)NCC4=C(C=CC5=C4CCO5)F
Isomeric SMILES CC1=C(C=CC=N1)C2=CN=C(N3C2=NN=C3)NCC4=C(C=CC5=C4CCO5)F
PubChem CID 121412508
Molecular Weight 376.39

Certificates

Certificate of Analysis(COA)

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10 results found

Lot NumberCertificate TypeDateItem
B2426432Certificate of AnalysisJan 17, 2024 M414309
B2426448Certificate of AnalysisJan 17, 2024 M414309
B2426449Certificate of AnalysisJan 17, 2024 M414309
B2426450Certificate of AnalysisJan 17, 2024 M414309
B2426451Certificate of AnalysisJan 17, 2024 M414309
B2426452Certificate of AnalysisJan 17, 2024 M414309
B2426453Certificate of AnalysisJan 17, 2024 M414309
B2426454Certificate of AnalysisJan 17, 2024 M414309
B2426455Certificate of AnalysisJan 17, 2024 M414309
B2426468Certificate of AnalysisJan 17, 2024 M414309

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 12.5 mg/mL (33.21 mM); Water: Insoluble; Ethanol: Insoluble;

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