HDAC-IN-48 是一种强效的HDAC抑制剂，是具有细胞毒性的杂交分子。HDAC-IN-48 由 SAHA 和 CETZOLE 分子的药效团组成，可诱导铁死亡 (ferroptosis) 并抑制HDAC蛋白。
| 生物活性 | HDAC-IN-48 is a potentHDACinhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI50~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 inducesferroptosisand inhibitsHDACproteins[1]. |
体外研究
(In Vitro) | HDAC-IN-48 (0-40 μM; 3 d) has superior antiproliferative activity on cancer cells (NCI-H522 and HCT-116) vs the normal cells (WI38 and RPE) with IC50s of 0.5 μM (NCI-H522), 0.61 μM (HCT-116), 8.37 μM (WI38, normal human lung fibroblasts), and 6.13 μM (RPE, retinal pigment epithelial cells), respectively[1].
HDAC-IN-48 (2.5 μM; 24 h) suppresses cell viability by inducing ferroptosis and HDAC inhibition[1].
HDAC-IN-48 (10 μM; 6 h) decreases the lipid peroxide level compared with SAHA[1].
HDAC-IN (0.58 μM, 1.16 μM, and 2.32 μM; 3 d) has no neurotoxic effects and (2.5, 5, and 10 μM; 3 d) leads to hyper acetylation of histones and tubulin[1].
Nondifferentiated PC-12 cells have stem-like properties, but when differentiated by a nerve growth factor, they demonstrate neuronal behavior. HDAC-IN-48 (0.58 μM, 1.16 μM, and 2.32 μM; 24 h) behaves as the HDAC control effect, shows few ferroptosis induction on both differentiated and undifferentiated PC-12 cells[1].
Western Blot Analysis[1] | Cell Line: | NCI-H522 cells | | Concentration: | 2.5, 5, and 10 μM | | Incubation Time: | 72 hours; at the corresponding concentrations in the presence of Liproxstatin-1 (0.25 μM) | | Result: | Led to hyperacetylation of histones and tubulin in a similar way to SAHA (pan-inhibitor). |
Cell Viability Assay[1] | Cell Line: | NCI-H522, WI38, HCT-116, and RPE | | Concentration: | 0-40 μM | | Incubation Time: | 72 hours | | Result: | Showed selectivity among normal cells over cancer cells.
Inhibited cell survival with IC50s of 0.5 μM, 8.37 μM, 0.61 μM, and 6.13 μM. |
Apoptosis Analysis[1] | Cell Line: | NCI-H522 cells | | Concentration: | 5 μM | | Incubation Time: | 24 hours, 48 hours, and 72 hours | | Result: | Induced cell ferroptosis. |
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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. |
