PROTAC HDAC8 Degrader-2
PROTAC HDAC8 Degrader-2 is a HDAC6/8 PROTAC degrader, with IC50 values of 0.042 μM and 0.147 μM against human HDAC8 and HDAC6, respectively, and exhibits selectivity over other class I HDAC isozymes. PROTAC HDAC8 Degrader-2 induces apoptosis (apoptosis) in leukemia cells, shows no obvious cytotoxicity to normal cells, and has favorable chemical stability. PROTAC HDAC8 Degrader-2 can be used in research related to acute myeloid leukemia.
(Pink: hHDAC6 and hHDAC8 ligand (HY-103596); Blue: Cereblon ligand (HY-103596); Black: linker).
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: C39H44N10O8
- 分子量:780.83
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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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[1]|
hHDAC1 0.029 μM (IC50) |
hHDAC2 0.141 μM (IC50) |
hHDAC3 0.059 μM (IC50) |
hHDAC6 0.147 μM (IC50) |
hHDAC8 0.042 μM (IC50) |
hHDAC1 81.6 nM (DC50) |
hHDAC2 217.6 nM (DC50) |
hHDAC3 64.6 nM (DC50) |
hHDAC6 14.3 nM (DC50) |
hHDAC8 8.98 nM (DC50) |
体外実験
PROTAC HDAC8 Degrader-2 (32a) inhibits recombinant human HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, with IC50 values of 0.029 μM, 0.141 μM, 0.059 μM, 0.147 μM and 0.042 μM, respectively[1].
PROTAC HDAC8 Degrader-2 (7.8-1000 nM; 24 h) induces dose-dependent degradation of HDAC1, HDAC2, HDAC3, HDAC8 and HDAC6 in MV-4-11 cells via the ubiquitin-proteasome system, with the highest potency against HDAC8 (DC50 = 8.98 nM) and HDAC6 (DC50 = 14.3 nM)[1].
PROTAC HDAC8 Degrader-2 (12.5-200 nM; 24 h) induces dose-dependent apoptosis in MV-4-11 leukemia cells[1].
PROTAC HDAC8 Degrader-2 (50 μM; 24 h) exhibits no significant cytotoxicity in HEK293 cells[1].
PROTAC HDAC8 Degrader-2 maintains 96% chemical stability following a 72 h incubation[1].
PROTAC HDAC8 Degrader-2 (10 μM; 5 min-6 h) exhibits favorable plasma stability in human pooled plasma, with 61% of the compound remaining after incubation at 37 °C for 6 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 leukemic cells
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Concentration:7.8, 15.5, 31.2, 62.5, 125, 250,500 and 1000 nM (HDAC1/2/3/8 degradation);0.78, 1.56, 3.13, 6.25,12.5, 25, 50 and 100 nM (HDAC6 DC₅₀ determination 250, 500 and 1000 nM (HDAC2/HDAC1/HDAC3 degradation); 50 and 500 nM (co-treatment with inhibitors)
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Incubation Time:24 h
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Result:Induced 49.6% degradation of HDAC2 at 1 μM.
Nearly completely degraded HDAC3 and induced 65.5% degradation of HDAC1 at 250 nM.
Degraded HDAC8 and HDAC6 at concentrations as low as 12.5 nM, with 75.8% degradation of HDAC8 and 33.9% degradation of HDAC6 at this dose.
Yielded DC50 values of 8.98 nM for HDAC8, 81.6 nM for HDAC1, 217.6 nM for HDAC2, 64.6 nM for HDAC3, and 14.3 nM for HDAC6.
Reversed degradation when co-treated with proteasome inhibitors or neddylation inhibitor MLN4924, confirming reliance on the ubiquitin-proteasome system.
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Cell Line:MV-4-11 leukemic cells
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Concentration:12.5, 25, 50, 100, 150 and 200 nM
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Incubation Time:24 h
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Result:Induced 11.32% apoptosis at 12.5 nM.
Induced 11.67% apoptosis at 25 nM.
Induced 21.03% apoptosis at 50 nM.
Induced 59.44% apoptosis at 100 nM.
Induced 75.05% apoptosis at 150 nM.
Induced 75.16% apoptosis at 200 nM.
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Cell Line:human HEK293 normal cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Showed no significant cytotoxicity against HEK239 cells, with a cell viability of 67.4% at 50 μM.
化学情報
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分子量 780.83
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分子式 C39H44N10O8
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SMILES
O=C(C1=CN=C(N2CCN(CC3=CN(C)C4=C3C=C(OCC(NCCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)C=C4)CC2)N=C1)NO
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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)
PROTAC HDAC8 Degrader-2 関連分類
HY-168175 関連分類
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