MilliporeSigma™ Calbiochem™ Autotaxin Inhibitor II, HA130

Description

A thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC₅₀ ∽28nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinet

A thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC₅₀ ∽28nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinetics. Reported to exhibit low cytotoxicity (TD₅₀ = 83, 105, and 2056μM in HEK293T, A2058, and HepG2 cultures) and no activity toward NPP1, PDE, AP, or proteasomal chymotryptic/tryptic/caspase-like activities even at concentrations as high as 10μM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463μg/kg, i.v.) in vivo , the effect appears short-lived as is the case with S32826 (Cat. No. 189510).

Specifications

• Color: Off-white
• Description: 97% by HPLC
• Molecular Formula: C₂₄H₁₉BFNO₅S
• Formula Weight: 463.3g/mol
• Solubility: DMSO
• Content And Storage: Hygroscopic, Protect from light
• Form: Solid
• Quantity: 10 mg