SAHA-OH 是一种选择性的HDAC6抑制剂 (IC50=23 nM)，与 HDAC1、2、3 和 8 相比，其对 HDAC6 有 10-47 倍的选择性。SAHA-OH 具有抗炎活性，并可减少巨噬细胞的凋亡。
| 生物活性 | SAHA-OH is a selectiveHDAC6inhibitor (IC50=23 nM), shows a 10- to 47-fold selectivity forHDAC6compared toHDAC1, 2, 3, and 8. SAHA-OH shows anti-inflammatory activity, and attenuates macrophageapoptosis[1]. |
| IC50& Target[1] | HDAC6 23 nM (IC50) | HDAC1 237 nM (IC50) | HDAC3 359 nM (IC50) | HDAC2 399 nM (IC50) | HDAC8 1070 nM (IC50) |
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体外研究
(In Vitro) | SAHA-OH (0.67-10.76 μM; 51 h) shows inhibition in bone marrow macrophages[1].
SAHA-OH (0.01 μM; 3 h) treatment in BMMOs (bone marrow macrophages) reduces IL-6, TNFα, IFNβ, IL-1β, IL-10, MCP-1 (CCL2) and GROα (CXCL1) secretions[1].
SAHA-OH (10 μM; 4 or 9 h) treatment induces acetylation of cytoplasmic α-tubulin and nuclear histone H3[1].
SAHA-OH (0-30 μM; 3 h) treatment attenuates macrophage apoptosis[1].
SAHA-OH (0-30 μM; 3 h) treatment attenuates B cell death[1].
Cell Viability Assay[1] | Cell Line: | BMMOs (bone marrow macrophages) | | Concentration: | 0.67-10.76 μM | | Incubation Time: | 51 h | | Result: | Showed IC50value in unstimulated BMMOs of 1.26 μM, and showed IC50value in LPS-stimulated BMMOs of 10.76 μM. |
Apoptosis Analysis[1] | Cell Line: | BMMOs (bone marrow macrophages) | | Concentration: | 0-30 μM | | Incubation Time: | 3 h | | Result: | Resulted in a 24- to 26-fold increase in cellular viability as compared to the SAHA treatment. |
Cell Cytotoxicity Assay[1] | Cell Line: | B cells | | Concentration: | 0-30 μM | | Incubation Time: | 3 h | | Result: | Resulted in a 5-fold enhancement in viability and a 3-fold decrease in cell death for the B cell population. |
Western Blot Analysis[1] | Cell Line: | BMMOs (bone marrow macrophages) | | Concentration: | 10 μM | | Incubation Time: | 4 or 9 h | | Result: | Resulted in the acetylation of α-tubulin.
Induced the acetylation of histone H3 compared to no treatment (NT). |
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体内研究
(In Vivo) | SAHA-OH (intraperitoneal injection; 50 mg/kg; once) treatment prevents splenic organ damage, and reduces plasma proinflammatory cytokine levels in LPS-induced endotoxemia mouse model[1].
| Animal Model: | LPS-induced endotoxemia mouse model[1] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection; 50 mg/kg; once | | Result: | Reduced proinflammatory cytokine secretions by about 50% compared to no treatment (NT) control mice.
Showed similar architecture as no treatment (NT) control and displayed well-organized lymphoid follicles. |
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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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