1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Ferroptosis
  3. HDAC-IN-48

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。HDAC-IN-48 是一种点击化学试剂。它含有 Alkyne 基团,可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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HDAC-IN-48 Chemical Structure

HDAC-IN-48 Chemical Structure

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  • 生物活性

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生物活性

HDAC-IN-48 is a potent HDAC inhibitor. 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 induces ferroptosis and inhibits HDAC proteins[1]. HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

295.36

Formula

C13H17N3O3S

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.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HDAC-IN-48
目录号:
HY-151872
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