HDAC-IN-94
HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3/10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C18H18N2O5
- 分子量:342.35
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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生物活性
製品説明
IC50 & Target
[1]|
hHDAC6 4.5 nM (IC50) |
hHDAC8 3273 nM (IC50) |
hHDAC1 403 nM (IC50) |
hHDAC10 202 nM (IC50) |
hHDAC2 537 nM (IC50) |
hHDAC3 1278 nM (IC50) |
hHDAC5 4455 nM (IC50) |
hHDAC11 >10000 nM (IC50) |
体外実験
HDAC-IN-94 (compound 5o) fits within the catalytic site of hHDAC6 with the hydroxamic acid group, modelled in neutral form, able to chelate the zinc atom, and its polar benzamide hydrogen forming a hydrogen bond with Ser568[1].
HDAC-IN-94 (1-10 μM, 24 h) promotes acetylation of α-tubulin in a dose-dependent manner in SH-SY5Y cells[1].
HDAC-IN-94 (10 nM-30 μM, 24-72 h) shows no cytotoxicity in HEK-293 cells at concentrations up to 30 μM[1].
HDAC-IN-94 (24-72 h) shows antiproliferation activity against U87-MG, T98G, U251-MG and SH-SY5Y cells, with IC50s of 51.31, 42.60, 2.37, and 3.32 μM, respectively[1].
HDAC-IN-94 (3 μM, 24 h) promotes G2/M cell cycle arrest, triggers programmed cell death, and induces a minor autophagy stimulation in SH-SY5Y cells[1].
HDAC-IN-94 (3-30 μM, 24-72 h) demonstrates a clear time- and concentration-dependent pro-apoptotic activity in SH-SY5Y cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells
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Concentration:1 and 10 μM
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Incubation Time:24 h
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Result:Promoted acetylation of α-tubulin in a dose-dependent manner.
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Cell Line:SH-SY5Y cells
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Concentration:3 μM
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Incubation Time:24 h
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Result:Led to an accumulation of hypodiploid SH-SY5Y cells in the subG0/G1 phase.
Showed a decrease in the G0/G1 population and a slight increase in cells within the S-phase.
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Cell Line:SH-SY5Y cells
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Concentration:3, 10, and 30 μM
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Incubation Time:24, 48 and 72 h
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Result:Induced a concentration-dependent increase in early apoptosis at 24 h.
Induced a significant increase of late apoptosis starting at 10 μM (24 h).
Showed significant effects on both early and late apoptosis at 10 μM and a pronounced apoptotic response at 30 μM (46 % for early and 27 % for late apoptosis), at 48 h of treatment.
Significantly increased early and late apoptosis at all concentrations at 72 h.
Induced a concentration-dependent increase in caspase-3/7 activation, starting from 10 μM at 24 h.
Elicited 24% caspase-positive cells at 30 μM at 24 h.
Showed a significant increase in caspase activation at 10 μM and 30 μM at 48 h.
Continued to activate caspase-3/7 in a concentration-dependent manner after 72 h, with 43% positivity at 30 μM.
化学情報
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分子量 342.35
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分子式 C18H18N2O5
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SMILES
O=C(NCC1=CC=C(C(NO)=O)C=C1)/C=C/C2=CC(OC)=C(O)C=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
HDAC-IN-94 関連分類
HY-179019 関連分類
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