An inhibitor of ADAM17/TACE

TMI-005 – 10 mg

Brand:
Cayman
CAS:
287405-51-0
Storage:
-20
UN-No:
Non-Hazardous - /

TMI-005 is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17/TNF-α converting enzyme (ADAM17/TACE), matrix metalloproteinase-1 (MMP-1), and MMP-13 (IC50s = 20, 33, and 8.1 nM, respectively).{45590} It inhibits LPS-induced TNF-α release in isolated human whole blood (IC50 = 144 ng/ml).{45591} TMI-005 (25 μM) reduces basal and ionizing radiation-induced secretion of the ADAM17/TACE substrates ALCAM and amphiregulin from A549 and NCI H125 cells.{45592} It inhibits proliferation of A549 cells when used at concentrations of 25 and 50 μM and sensitizes A549 and NCI H125 cells to ionizing radiation at 25 μM. TMI-005 (25 mg/kg twice per day) reduces tumor growth in an A549 mouse xenograft model when administered in combination with ionizing radiation.  

 

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SKU: 29016 - 10 mg Category:

Description

An inhibitor of ADAM17/TACE, MMP-1, and MMP-13 (IC50s = 20, 33, and 8.1 nM, respectively); inhibits LPS-induced TNF-α release in isolated human whole blood (IC50 = 144 ng/ml); reduces basal and ionizing radiation-induced secretion of ALCAM and amphiregulin from A549 and NCI H125 cells at 25 μM; inhibits proliferation of A549 at 25 and 50 μM; sensitizes A549 and NCI H125 cells to ionizing radiation at 25 μM; reduces tumor growth in an A549 mouse xenograft model when administered at 25 mg/kg twice per day in combination with ionizing radiation

Formal name: (3S)-N-hydroxy-4-[[4-[(4-hydroxy-2-butyn-1-yl)oxy]phenyl]sulfonyl]-2,2-dimethyl-3-thiomorpholinecarboxamide

Synonyms:  Apratastat

Molecular weight: 414.5

CAS: 287405-51-0

Purity: ≥98%

Formulation: A crystalline solid

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