R-minus-Gossypol-acetic-acid-AT-101-acetic-acid-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE(R)-(-)-Gossypol acetic acidCat. No.: HY-15464ACAS No.: 866541-93-7Synonyms: AT-101 (acetic acid); (-)-Gossypol acetic acid; (R)-Gossypolacetic acid分式: CHO分量: 578.61作靶點(diǎn): Bcl-2 Family; Autophagy作通路: Apoptosis; Autophagy儲(chǔ)存式: -20C,

2、 protect from light, stored under argon* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight, stored under argon)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 39.33 mg/mL (67.97 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.7283 mL 8.6414 mL 17.2828 mL5 mM 0.3457 mL 1.7283 mL 3.4

3、566 mL10 mM 0.1728 mL 0.8641 mL 1.7283 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)是天然產(chǎn)物 Gossypol 的左旋異構(gòu)體。AT-101 結(jié)合到 Bcl-2，Mcl-1 和 Bcl-xL 蛋，Ki 值分別為 26030 nM，17010 nM 和 48040 nM。IC50 & Target Bcl-2 Bcl-xL Mcl-1 Autophagy260 nM

4、(Ki) 480 nM (Ki) 170 nM (Ki)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 The natural racemic Gossypol has two enantiomers, namely the (R)-(-)-Gossypol acetic acid (AT-101 (aceticacid) and (+)-Gossypol enantiomers. (R)-(-)-Gossypol (AT-101) and (+)-Gossypol binds to Bcl-2 or Bcl-xLwith simil

5、ar binding affinities, AT-101 is more potent than (+)-Gossypol in inhibition of cell growth andinduction of apoptosis, possibly due to the influence of serum in the cell culture experiments. The racemicform and each of the enantiomers of Gossypol are tested against UM-SCC-6 and UM-SCC-14A in 6-dayMT

6、T assays. (R)-(-)-Gossypol (AT-101) exhibits greater growth inhibition relative to ()-Gossypol than (+)-Gossypol in both cell lines tested (P50 of 2-5 M and a less sensitive group with IC50 clusters around 10 M1. (R)-(-)-Gossypol (AT-101) is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins wit

7、h Ki values of26030 nM, 17010 nM, and 48040 nM, respectively 2.PROTOCOLCell Assay 1 Two representative UM-SCC cell lines, UM-SCC-6 and UM-SCC-14A, are continuously exposed to 0 (vehiclecontrol), 5 or 10 M ()-Gossypol, (R)-(-)-Gossypol (AT-101) or (+)-Gossypol in a 6-day MTT cell survivalassay 1.MCE

8、has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cancer Lett. 2019 Jul 10;461:31-43.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Oliver CL, et al. In vitro effects of the BH3 mimetic, (-)-Gossypol, on head and neck squamo

9、us cell carcinoma cells. Clin Cancer Res.2004 Nov 15;10(22):7757-63.2. Sun Y, et al. Apogossypolone, a nonpeptidic small molecule inhibitor targeting Bcl-2 family proteins, effectively inhibits growth of diffuselarge cell lymphoma cells in vitro and in vivo. Cancer Biol Ther. 2008 Sep;7(9):1418-26.McePdfHeightCaution: Product has not been fully validated for medic