CPTH2 hydrochloride 是有效的组蛋白乙酰基转移酶 (HAT) 抑制剂。CPTH2 hydrochloride 选择性地抑制Gcn5对组蛋白 H3 的乙酰化。CPTH2 hydrochloride 通过抑制乙酰转移酶p300 (KAT3B)诱导凋亡 (apoptosis) 并降低透明细胞肾癌 (ccRCC) 细胞系的侵袭性。
| 生物活性 | CPTH2 hydrochloride is a potenthistone acetyltransferase(HAT)inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 byGcn5. CPTH2 hydrochloride inducesapoptosisand decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition ofacetyltransferase p300 (KAT3B)[1][2]. |
| IC50& Target[1][2] | |
体外研究
(In Vitro) | CPTH2 (100 μM; 12, 24, 48 hours) hydrochloride causes a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation[1].
CPTH2 (100 μM; 12 or 48 hours) hydrochloride causes a comparable drop of the activity in both cell lines[1].
CPTH2 (100 μM; 48 hours) hydrochloride produces a drastic increase in apoptotic/dead cell population after 48 h[1].
CPTH2 (100 μM; 12, 24, 48 hours) hydrochloride shows a reduced acetylation of both global AcH3 histone and H3AcK18[1].
CPTH2 (100 μM; 24, 48 hours) hydrochloride is capable to counteract invasion and migration of ccRCC-786-O cells in culture[1].
CPTH2 (0.2, 0.5, 1 mM) hydrochloride inhibits the growth of a GCN5 deleted strain and a single catalytic mutant E173H[2].
CPTH2 (0.6, 0.8 mM; for 24 hours) hydrochloride inhibits histone H3 acetylation in yeast cell cultures[2].
CPTH2 hydrochloride inhibits the Gcn5p dependent functional network[2].
Cell Proliferation Assay[1] | Cell Line: | Papillary thyroid (K1) and clear cell Renal Cell Carcinoma (ccRCC-786-O) cell lines | | Concentration: | 100 μM | | Incubation Time: | 12, 24, 48 hours | | Result: | Caused a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation. |
Cell Viability Assay[1] | Cell Line: | K1 and ccRCC-786-O cell lines | | Concentration: | 100 μM | | Incubation Time: | 24 hours (K1 cell) and 48 hours (ccRCC-786-O cell) | | Result: | Caused a comparable drop of the activity in both cell lines. |
Apoptosis Analysis[1] | Cell Line: | ccRCC-786-O cells | | Concentration: | 100 μM | | Incubation Time: | 48 hours | | Result: | Produced a drastic increase in apoptotic/dead cell population after 48 h. |
Western Blot Analysis[1] | Cell Line: | ccRCC-786-O cells | | Concentration: | 100 μM | | Incubation Time: | 12, 24, 48 hours | | Result: | Showed a reduced acetylation of both global AcH3 histone and H3AcK18. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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