Garcinol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Garcinol (Camboginol) 是体外和体内组蛋白乙酰转移酶 (HAT) p300 (IC50=7 uM) 和 PCAF (IC50=5 uM) 的有效天然抑制剂。

Garcinol (Camboginol) is a potent, natural inhibitor of histone acetyltransferases (HATs) p300 (IC50=7 uM) and PCAF (IC50=5 uM) both in vitro and in vivo; downregulates various cell survival proteins including survivin, bcl-2, XIAP, and cFLIP, and induces bid cleavage, bax, and cytochrome c release, potentiates TRAIL-induced apoptosis through upregulation of death receptors and downregulation of antiapoptotic proteins; also siimulates neurogenesis and ex vivo expansion of human hematopoietic stem cells.

Garcinol (10-50 μM; 24-72 hours) can inhibit the proliferation of two HNSCC cell lines tested (CAL27 and UMSCC1) in a time- and dose-dependent manner. Garcinol (10-50 μM; 24-72 hours) induces apoptosis in HNSCC cells. Garcinol (50 μM; 1-6 hours) suppresses phosphorylation and degradation of the constitutive IκBα in a time-dependent manner. Cell Proliferation Assay Cell Line:CAL27 and UMSCC1 cells Concentration:10, 25, 50 μM Incubation Time:24, 48, and 72 hours Result:Inhibited the proliferation of two HNSCC cell lines in a time- and dose-dependent manner. Apoptosis Analysis Cell Line:CAL27 and UMSCC1 cells Concentration:10, 25, 50 μM Incubation Time:24, 48, and 72 hours Result:Induced apoptosis in HNSCC cells.Western Blot Analysis Cell Line:CAL27 cells Concentration:50 μM Incubation Time:1, 2, 4, 6 hours Result:Suppressed phosphorylation and degradation of the constitutive IκBα in a time-dependent manner.

Garcinol (i.p.; 1 and 2 mg/kg; five times/week for 4 consecutive weeks) induces significant inhibition of tumor growth. Animal Model:Five-week-old athymic nu/nu male mice bearing subcutaneous CAL27 tumors Dosage:1 and 2 mg/kg Administration:I.p.; five times/week for 4 consecutive weeks Result:Induced significant inhibition of tumor growth.

Camboginol

Chromatin/Epigenetic

HAT

HAT

——

——

78824-30-3

602.812

C38H50O6

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (82.95 mM)

CC(=CCC1CC2(C(=O)C(=C(C3=CC(=C(C=C3)O)O)O)C(=O)C(C2=O)(C1(C)C)CC=C(C)C)CC(CC=C(C)C)C(=C)C)C

3-(3,4-dihydroxybenzoyl)-4-hydroxy-8,8-dimethyl-1,7-bis(3-methyl-2-buten-1-yl)-5-[(2S)-5-methyl-2-(1-methylethenyl)-4-hexen-1-yl]-bicyclo[3.3.1]non-3-ene-2,9-dione

(-20℃)

With Ice Pack

≥ 2 years