Cas No.: | 338967-87-6 |
Chemical Name: | 4(1H)-Quinazolinone,3-(2,4-dichloro-5-methoxyphenyl)-2,3-dihydro-2-thioxo- |
Synonyms: | 4(1H)-Quinazolinone, 3-(2,4-dichloro-5-methoxyphenyl)-2,3-dihydro-2-thioxo-;Mdivi-1;3-(2,4-Dichloro-5-methoxyphenyl)-2,3-dihydro-2-thioxo-4(1H)-quinazolinone;3-(2,4-dichloro-5-methoxyphenyl)-2-sulfanylidene-1H-quinazolin-4-one;Mdivi 1;HMS575G09;Mitochondrial division inhibitor 1;3-(2,4-Dichloro-5-methoxyphenyl)-2-sulfanyl-4(3H)-quinazolinone;3-(2,4-Dichloro-5-methoxyphenyl)-2-thioxo-2,3-dihydro-4(1H)-quinazolinone |
SMILES: | O=C1N(C2=C(Cl)C=C(Cl)C(OC)=C2)C(S)=NC3=C1C=CC=C3 |
Formula: | C15N2O2Scl2H10 |
M.Wt: | 353.2231 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor. |
In Vivo: | The mitochondrial division DRP, Dnm1, is the target of mdivi-1 in vivo. Mdivi-1 quantitatively blocks GMPPCP- dependent Dnm1 self-assembly in a concentration range similar to its effects on mitochondrial division in vivo[1]. Mdivi-1 (50 mg/kg, i.p.) significantly decreases GFAP protein expression in the normal mouse retina[3]. |
In Vitro: | Mdivi-1 inhibits Dnm1 GTPase activity in a dose-dependent manner, with an estimated EC50 of 1-10 μM. Mdivi-1 increases the apparent K0.5 for GTP, lowers the apparent Vmax for GTP hydrolysis, and causes an increase in the Hill coefficient observed for GTP in the Dnm1 GTP hydrolysis reaction[1]. Cells treated with mdivi-1 display decreased cytochrome c release and a reduced rate of phosphatidylserine exposure on their surface following apoptosis induction, consistent with an inhibition of apoptosis and with previous studies using other strategies to compromise DRP1 activity[2]. Mdivi-1 results in apoptotic cell death in ischemic retina[3]. |