Grouped product items

SKU

Size

Availability

Price

Qty

G286917-1mg

1mg

Available within 4-8 weeks(?)

$37.90

G286917-5mg

5mg

Available within 4-8 weeks(?)

$154.90

G286917-10mg

10mg

In stock

$199.90

G286917-25mg

25mg

Available within 4-8 weeks(?)

$578.90

G286917-50mg

50mg

In stock

$699.90

Basic Description

Synonyms	GSK2239633A\|1240516-71-5\|GSK 2239633A\|GSK-2239633A\|GSK-2239633\|07ODS257BP\|CHEMBL2018969\|N-((3-((3-((5-Chloro-2-thienyl)sulfonylamino)-4-methoxy-indazol-1-yl)methyl)phenyl)methyl)-2-hydroxy-2-methyl-propanamide\|N-[[3-[[3-[[(5-Chloro-2-thienyl)sulfonyl]amin
Specifications & Purity	Moligand™, ≥98%(HPLC)
Biochemical and Physiological Mechanisms	Potent CCR4 antagonist (pIC50= 7.83 in a35S-GTPγS competition assay). Inhibits thymus activation-regulated chemokine (TARC) -induced F-actin polymerization in human whole blood.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ANTAGONIST
Mechanism of action	Antagonist of CCR4;Antagonist of CCR5
Product Description	GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96 ± 0.11.

Associated Targets

CXCR2 Tchem C-X-C chemokine receptor type 2 0 Activities

Discover Target: CXCR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CXCR4 Tclin C-X-C chemokine receptor type 4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CX3CR1 Tchem CX3C chemokine receptor 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CXCR3 Tchem C-X-C chemokine receptor type 3 0 Activities

Discover Target: CXCR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CXCR1 Tchem C-X-C chemokine receptor type 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GPR35 Tchem G-protein coupled receptor 35 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CCR2 Tchem C-C chemokine receptor type 2 0 Activities

Discover Target: CCR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CCR4 Tclin C-C chemokine receptor type 4 3 Activities

Discover Target: CCR4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CCR5 Tclin C-C chemokine receptor type 5 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CCR1 Tchem C-C chemokine receptor type 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CCR8 Tchem C-C chemokine receptor type 8 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CCR10 Tchem C-C chemokine receptor type 10 0 Activities

Discover Target: CCR10

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Discover Target: CDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FFAR4 Tchem Free fatty acid receptor 4 0 Activities

Discover Target: FFAR4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FPR2 Tchem N-formyl peptide receptor 2 0 Activities

Discover Target: FPR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 1 Activities

Discover Target: SLCO1B1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

S1PR1 Tclin Sphingosine 1-phosphate receptor 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

C5AR1 Tclin C5a anaphylatoxin chemotactic receptor 1 0 Activities

Discover Target: C5AR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRB2 Tclin Beta-2 adrenergic receptor 0 Activities

Discover Target: ADRB2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRNA1 Tclin Acetylcholine receptor subunit alpha 0 Activities

Discover Target: CHRNA1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

APLNR Tchem Apelin receptor 0 Activities

Discover Target: APLNR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

Discover Target: ADRA2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADGRF1 Tbio Adhesion G-protein coupled receptor F1 0 Activities

Discover Target: ADGRF1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AGTR1 Tclin Type-1 angiotensin II receptor 0 Activities

Discover Target: AGTR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Discover Target: GSK3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GPR119 Tclin Glucose-dependent insulinotropic receptor 0 Activities

Discover Target: GPR119

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GLP1R Tclin Glucagon-like peptide 1 receptor 0 Activities

Discover Target: GLP1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Discover Target: MAPK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide
INCHI	InChI=1S/C24H25ClN4O5S2/c1-24(2,31)23(30)26-13-15-6-4-7-16(12-15)14-29-17-8-5-9-18(34-3)21(17)22(27-29)28-36(32,33)20-11-10-19(25)35-20/h4-12,31H,13-14H2,1-3H3,(H,26,30)(H,27,28)
InChi Key	YTEVTHHGQMUPHC-UHFFFAOYSA-N
Canonical SMILES	CC(C)(C(=O)NCC1=CC(=CC=C1)CN2C3=C(C(=CC=C3)OC)C(=N2)NS(=O)(=O)C4=CC=C(S4)Cl)O
Isomeric SMILES	CC(C)(C(=O)NCC1=CC(=CC=C1)CN2C3=C(C(=CC=C3)OC)C(=N2)NS(=O)(=O)C4=CC=C(S4)Cl)O
PubChem CID	46861584
Molecular Weight	549.06

Database links

PubChem CID	46861584
CAS Registry No.	1240516-71-5
ChEMBL Ligand	CHEMBL2018969
BindingDB Ligand	50380880
GPCRdb Ligand	GSK2239633A

Certificates

Certificate of Analysis(COA)

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7 results found

Lot Number	Certificate Type	Date	Item
K2316172	Certificate of Analysis	Nov 07, 2023	G286917
K2316173	Certificate of Analysis	Nov 07, 2023	G286917
K2316336	Certificate of Analysis	Nov 07, 2023	G286917
K2316337	Certificate of Analysis	Nov 07, 2023	G286917
K2316338	Certificate of Analysis	Nov 07, 2023	G286917
K2316339	Certificate of Analysis	Nov 07, 2023	G286917
K2316340	Certificate of Analysis	Nov 07, 2023	G286917

Chemical and Physical Properties

Solubility	Solvent:DMSO, Max Conc. mg/mL: 54.91, Max Conc. mM: 100

References

1. Procopiou PA, Barrett JW, Barton NP, Begg M, Clapham D, Copley RC, Ford AJ, Graves RH, Hall DA, Hancock AP et al.. (2013) Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.. J Med Chem, 56 (5): (1946-60). [PMID:23409871]
2. Cahn A, Hodgson S, Wilson R, Robertson J, Watson J, Beerahee M, Hughes SC, Young G, Graves R, Hall D et al.. (2013) Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study.. BMC Pharmacol Toxicol, 14 (3): (14). [PMID:23448278]

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SKU	Size	Availability	Price
G286917-1mg	1mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$37.90
G286917-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$154.90
G286917-10mg	10mg	In stock	$199.90
G286917-25mg	25mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$578.90
G286917-50mg	50mg	In stock	$699.90

GSK 2239633A - ≥98%(HPLC), high purity , CAS No.1240516-71-5, Antagonist of CCR4;Antagonist of CCR5

Basic Description

Associated Targets

CXCR2 Tchem C-X-C chemokine receptor type 2 0 Activities

CXCR4 Tclin C-X-C chemokine receptor type 4 0 Activities

CX3CR1 Tchem CX3C chemokine receptor 1 0 Activities

CXCR3 Tchem C-X-C chemokine receptor type 3 0 Activities

CXCR1 Tchem C-X-C chemokine receptor type 1 0 Activities

GPR35 Tchem G-protein coupled receptor 35 0 Activities

CCR2 Tchem C-C chemokine receptor type 2 0 Activities

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

CCR4 Tclin C-C chemokine receptor type 4 3 Activities

CCR5 Tclin C-C chemokine receptor type 5 0 Activities

CCR1 Tchem C-C chemokine receptor type 1 0 Activities

CCR8 Tchem C-C chemokine receptor type 8 0 Activities

CCR10 Tchem C-C chemokine receptor type 10 0 Activities

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

FFAR4 Tchem Free fatty acid receptor 4 0 Activities

FPR2 Tchem N-formyl peptide receptor 2 0 Activities

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 1 Activities

S1PR1 Tclin Sphingosine 1-phosphate receptor 1 0 Activities

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

C5AR1 Tclin C5a anaphylatoxin chemotactic receptor 1 0 Activities

BRPF1 Tchem Peregrin 0 Activities

AURKA Tchem Aurora kinase A 0 Activities

ADRB2 Tclin Beta-2 adrenergic receptor 0 Activities

CHRNA1 Tclin Acetylcholine receptor subunit alpha 0 Activities

APLNR Tchem Apelin receptor 0 Activities

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

ADGRF1 Tbio Adhesion G-protein coupled receptor F1 0 Activities

AGTR1 Tclin Type-1 angiotensin II receptor 0 Activities

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

GPR119 Tclin Glucose-dependent insulinotropic receptor 0 Activities

GLP1R Tclin Glucagon-like peptide 1 receptor 0 Activities

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Chemical and Physical Properties

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References

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