GSK-199 hydrochloride | B1037

GSK-199 is a potent, reversible inhibitor of PAD4 (IC₅₀ = 200 nM. It binds to the low-calcium form of the enzyme and is selective for PAD4 over PAD1-3. It is less potent than the related PAD4 inhibitor GSK484 (IC₅₀ = 50 nM). GSK-199 can inhibit the citrullination of PAD4 target proteins and diminish the formation of neutrophil extracellular traps in mouse neutrophils.

GSK-199 is a potent, reversible inhibitor of PAD4 (IC₅₀ = 200 nM. It binds to the low-calcium form of the enzyme and is selective for PAD4 over PAD1-3. It is less potent than the related PAD4 inhibitor GSK484 (IC₅₀ = 50 nM). GSK-199 can inhibit the citrullination of PAD4 target proteins and diminish the formation of neutrophil extracellular traps in mouse neutrophils.

B1037 | GSK-199 hydrochloride DataSheet

Alternate Name/Synonyms: (R)-(3-Aminopiperidin-1-yl)(2-(1-ethyl-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride

Appearance: Crystalline solid

Formulation: N/A

CAS Number: 1549811-53-1

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₄H₂₉ClN₆O₂

Molecular Weight: 468.98

Cell-Permeable?: Yes

Purity: ≥98%

Solubilities: DMSO (~30 mg/ml)

Handling: Protect from air and moisture

Country of Origin: USA

Tag Line: A potent, reversible inhibitor of PAD4

MDL Number: N/A

PubChem CID: N/A

SMILES: O=C(N1C[C@H](N)CCC1)C2=CC(OC)=C3N(C)C(C4=CC5=CC=CN=C5N4CC)=NC3=C2.[H]Cl

InChi: InChI=1S/C24H28N6O2.ClH/c1-4-30-19(12-15-7-5-9-26-22(15)30)23-27-18-11-16(13-20(32-3)21(18)28(23)2)24(31)29-10-6-8-17(25)14-29;/h5,7,9,11-13,17H,4,6,8,10,14,25H2,1-3H3;1H/t17-;/m1./s1

InChi Key: KRGMIOKDGHBYQE-UNTBIKODSA-N