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GCN2-IN-6 - 99%, high purity , CAS No.2183470-09-7

COA

Grade & Purity:

≥99%

Cas Number: 2183470-09-7
Molecular Weight: 485.29
PubChem CID: 137347437

In stock

Item Number

G647478

Grouped product items
SKU	Size	Availability	Price
G647478-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$350.90
G647478-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$550.90
G647478-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,650.90
G647478-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$2,800.90

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Basic Description

Specifications & Purity	≥99%
Biochemical and Physiological Mechanisms	GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic ( IC 50 of 1.8 nM) and cellular assays ( IC 50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC 50 of 0.26 nM (in enzymatic assa
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.
Product Description	GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic ( IC 50 of 1.8 nM) and cellular assays ( IC 50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC 50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells) In Vitro To examine the impact of GCN2 inhibition on cancer cell proliferation, acute lymphoblastic leukemia (ALL) CCRFCEM cells are treated with GCN2-IN-6 (Compound 6d) in the presence of asparaginedepleting agent asparaginase. Treatment with GCN2-IN-6 greatly sensitizes CCRF-CEM cells to asparaginase. The moderate antiproliferative effects achieved by combining asparaginase and GCN2-IN-6 treatment are observed in GCN2-wildtype (WT) mouse embryonic fibroblast (MEF) cells but not in GCN2-knockout (KO) MEF.? GCN2-IN-6 demonstrates suppression on p-GCN2, p-eIF2α, and ATF4 activated by asparaginase. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GCN2-IN-6 (Compound 6d; 0.3-3 mg/kg; oral administration; for 8 hours; mice) treatment at 3 mg/kg suppresses both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice bearing CCRF-CEM cells xenografts Dosage: 0.3 mg/kg, 1 mg/kg, and 3 mg/kg Administration: Oral administration; for 8 hours Result: Suppressed both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase. Form:Solid IC50& Target:GCN2

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
- Superclass Benzenoids
  - Class Benzene and substituted derivatives
    - Subclass Sulfanilides

Kingdom	Organic compounds
Superclass	Benzenoids
Class	Benzene and substituted derivatives
Subclass	Sulfanilides
Intermediate Tree Nodes	Not available
Direct Parent	Sulfanilides
Alternative Parents	Benzenesulfonamides Benzenesulfonyl compounds Dichlorobenzenes Benzyl alcohols Fluorobenzenes Aminopyrimidines and derivatives Organosulfonamides Aryl fluorides Aryl chlorides Heteroaromatic compounds Aminosulfonyl compounds Azacyclic compounds Primary amines Primary alcohols Organopnictogen compounds Organofluorides Organochlorides Organic oxides Hydrocarbon derivatives Aromatic alcohols
Molecular Framework	Aromatic heteromonocyclic compounds
Substituents	Sulfanilide - Benzenesulfonamide - Benzenesulfonyl group - 1,4-dichlorobenzene - Benzyl alcohol - Halobenzene - Fluorobenzene - Chlorobenzene - Aminopyrimidine - Organosulfonic acid amide - Pyrimidine - Aryl halide - Aryl fluoride - Aryl chloride - Heteroaromatic compound - Aminosulfonyl compound - Sulfonyl - Organosulfonic acid or derivatives - Organic sulfonic acid or derivatives - Azacycle - Organoheterocyclic compound - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Aromatic alcohol - Primary amine - Primary alcohol - Organosulfur compound - Organooxygen compound - Organonitrogen compound - Organofluoride - Organochloride - Organohalogen compound - Amine - Alcohol - Aromatic heteromonocyclic compound
Description	This compound belongs to the class of organic compounds known as sulfanilides. These are organic aromatic compounds containing a sulfanilide moiety, with the general structure RS(=O)(=O)NC1=CC=CC=C1.
External Descriptors	Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61. DOI: 10.1186/s13321-016-0174-y

Names and Identifiers

IUPAC Name	N-[3-[2-(2-aminopyrimidin-5-yl)ethynyl]-2,4-difluorophenyl]-2,5-dichloro-3-(hydroxymethyl)benzenesulfonamide
INCHI	InChI=1S/C19H12Cl2F2N4O3S/c20-12-5-11(9-28)17(21)16(6-12)31(29,30)27-15-4-3-14(22)13(18(15)23)2-1-10-7-25-19(24)26-8-10/h3-8,27-28H,9H2,(H2,24,25,26)
InChIKey	VJXAWOQPYMAEFQ-UHFFFAOYSA-N
Smiles	C1=CC(=C(C(=C1NS(=O)(=O)C2=CC(=CC(=C2Cl)CO)Cl)F)C#CC3=CN=C(N=C3)N)F
PubChem CID	137347437
Molecular Weight	485.29

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

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

Analytical Chart:

Chemical and Physical Properties

Solubility	DMSO : 250 mg/mL (515.16 mM; Need ultrasonic)
Molecular Weight	485.300 g/mol
XLogP3	3.000
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	6
Exact Mass	483.998 Da
Monoisotopic Mass	483.998 Da
Topological Polar Surface Area	127.000 Å²
Heavy Atom Count	31
Formal Charge	0
Complexity	782.000
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

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