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

COA COA
In stock
Item Number
M414309
Grouped product items
SKU Size
Availability
 Price Qty
M414309-1mg
1mg
3
$29.90
M414309-5mg
5mg
3
$119.90
M414309-10mg
10mg
2
$189.90
M414309-25mg
25mg
2
$379.90
M414309-50mg
50mg
1
$599.90
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Histone Methyltransferase Inhibitors

View related series
embryonic ectoderm development Allosteric modulator (2) Epigenetics (1496) Histone Methyltransferase (190) Histone Modification (1379)

Basic Description

Synonyms A16922 | 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 & Purity Moligand™, ≥97%
Biochemical and Physiological Mechanisms 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.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type ALLOSTERIC MODULATOR
Mechanism of action Allosteric 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 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Triazolopyrimidines
Subclass Not available
Intermediate Tree Nodes Not available
Direct Parent Triazolopyrimidines
Alternative Parents Coumarans  Secondary alkylarylamines  Methylpyridines  Aminopyrimidines and derivatives  Alkyl aryl ethers  Benzenoids  Aryl fluorides  Triazoles  Heteroaromatic compounds  Oxacyclic compounds  Azacyclic compounds  Organopnictogen compounds  Organofluorides  Hydrocarbon derivatives  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Coumaran - Triazolopyrimidine - Methylpyridine - Secondary aliphatic/aromatic amine - Aminopyrimidine - Alkyl aryl ether - Benzenoid - Pyrimidine - Pyridine - Aryl halide - Aryl fluoride - Heteroaromatic compound - 1,2,4-triazole - Triazole - Azole - Oxacycle - Azacycle - Secondary amine - Ether - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Amine - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as triazolopyrimidines. These are polycyclic aromatic compounds containing triazole ring fused to a pyrimidine ring. Triazole is a five-membered ring consisting of two carbon atoms and three nitrogen atoms. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
External Descriptors Not available

Associated Targets(Human)

EED Tchem Polycomb protein EED (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC18A2 Tclin Synaptic vesicular amine transporter (118 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A5 Tclin Cytochrome P450 3A5 (525 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EED Tchem Polycomb protein EED (645 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Pde4d Phosphodiesterase 4D (4 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NIH3T3 (5395 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CT26 (928 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

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)
InChIKey XLIBABIFOBYHSV-UHFFFAOYSA-N
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
Molecular Weight 376.39
Reaxy-Rn 29638317
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29638317&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

10 results found

Lot Number Certificate Type Date Item
B2426449 Certificate of Analysis Jan 17, 2024 M414309
B2426450 Certificate of Analysis Jan 17, 2024 M414309
B2426432 Certificate of Analysis Jan 17, 2024 M414309
B2426448 Certificate of Analysis Jan 17, 2024 M414309
B2426451 Certificate of Analysis Jan 17, 2024 M414309
B2426452 Certificate of Analysis Jan 17, 2024 M414309
B2426453 Certificate of Analysis Jan 17, 2024 M414309
B2426454 Certificate of Analysis Jan 17, 2024 M414309
B2426455 Certificate of Analysis Jan 17, 2024 M414309
B2426468 Certificate of Analysis Jan 17, 2024 M414309

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 12.5 mg/mL (33.21 mM); Water: Insoluble; Ethanol: Insoluble;
Molecular Weight 376.400 g/mol
XLogP3 3.400
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 4
Exact Mass 376.145 Da
Monoisotopic Mass 376.145 Da
Topological Polar Surface Area 77.200 Ų
Heavy Atom Count 28
Formal Charge 0
Complexity 541.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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