GI254023X - 98% (HPLC), high purity , CAS No.260264-93-5, Inhibitor of ADAM10;Inhibitor of ADAM17

Item Number
G169107
Grouped product items
SKUSizeAvailabilityPrice Qty
G169107-1mg
1mg
In stock
$141.90
G169107-5mg
5mg
In stock
$218.90
G169107-10mg
10mg
In stock
$296.90
G169107-25mg
25mg
In stock
$573.90
G169107-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$890.90
G169107-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$1,385.90

Selective ADAM10 metalloprotease inhibitor

Basic Description

SynonymsGI4023 | AKOS025401993 | J-016226 | SCHEMBL11989235 | CCG-268545 | GI 254023X | (2r)-n-[(1s)-2,2-dimethyl-1-[(methylamino)carbonyl]-propyl]-2-[(1s)-1-[formyl(hydroxy)amino]ethyl]-5-phenylpentanamide | AC-27562 | Benzenepentanamide, N-[(1S)-2,2-dimethyl-1-
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsSelective ADAM10 metalloprotease inhibitor; displays over 100-fold higher potency at ADAM10 compared to ADAM17. Blocks constitutive release of IL-6R, CX3CL1 and CXCL16 in cell-based cleavage experiments. Inhibits calcium ionophore-induced betacellulin she
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of ADAM10;Inhibitor of ADAM17
Product Description

Product Application:

GI254023X has been used to inhibit ADAM10 (ADAM metallopeptidase domain 10).

Associated Targets(Human)

MMP1 Tchem Interstitial collagenase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MMP14 Tchem Matrix metalloproteinase-14 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MMP9 Tchem Matrix metalloproteinase-9 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MMP2 Tchem 72 kDa type IV collagenase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ADAM17 Tchem Disintegrin and metalloproteinase domain-containing protein 17 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ADAM10 Tchem Disintegrin and metalloproteinase domain-containing protein 10 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MMP14 Tchem Matrix metalloproteinase 14 (1592 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MMP1 Tchem Matrix metalloproteinase-1 (7046 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Adam17 ADAM17 (14 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mmp2 Matrix metalloproteinase-2 (12 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mmp9 Matrix metalloproteinase 9 (38 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 (2R)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-5-phenylpentanamide
INCHI InChI=1S/C21H33N3O4/c1-15(24(28)14-25)17(13-9-12-16-10-7-6-8-11-16)19(26)23-18(20(27)22-5)21(2,3)4/h6-8,10-11,14-15,17-18,28H,9,12-13H2,1-5H3,(H,22,27)(H,23,26)/t15-,17+,18+/m0/s1
InChi Key GHVMTHKJUAOZJP-CGTJXYLNSA-N
Canonical SMILES CC(C(CCCC1=CC=CC=C1)C(=O)NC(C(=O)NC)C(C)(C)C)N(C=O)O
Isomeric SMILES C[C@@H]([C@@H](CCCC1=CC=CC=C1)C(=O)N[C@H](C(=O)NC)C(C)(C)C)N(C=O)O
WGK Germany 3
PubChem CID 9952396
Molecular Weight 391.5

Certificates

Certificate of Analysis(COA)

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6 results found

Lot NumberCertificate TypeDateItem
A2211792Certificate of AnalysisOct 24, 2024 G169107
A2211796Certificate of AnalysisOct 24, 2024 G169107
A2211802Certificate of AnalysisOct 24, 2024 G169107
A2211860Certificate of AnalysisOct 24, 2024 G169107
A2211878Certificate of AnalysisOct 24, 2024 G169107
A2211880Certificate of AnalysisOct 24, 2024 G169107

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 7.83, Max Conc. mM: 20

Safety and Hazards(GHS)

WGK Germany 3

Related Documents

References

1. Ludwig A, Hundhausen C, Lambert MH, Broadway N, Andrews RC, Bickett DM, Leesnitzer MA, Becherer JD.  (2005)  Metalloproteinase inhibitors for the disintegrin-like metalloproteinases ADAM10 and ADAM17 that differentially block constitutive and phorbol ester-inducible shedding of cell surface molecules..  Comb Chem High Throughput Screen,  (2): (161-71).  [PMID:15777180] [10.1021/op500134e]

Solution Calculators