HDAC6-IN-13
Based on 1 Customer Validation
HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity.
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。
- 純度: 98.08%
- CAS 番号: 2837128-41-1
- 分子式: C23H22N4O
- 分子量:370.45
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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HDAC6 0.019 μM (IC50) |
HDAC3 1.03 μM (IC50) |
HDAC1 1.53 μM (IC50) |
HDAC2 2.06 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| J774.A1 | IC50 |
2.61 μM
Compound: 35m
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Antiinflammatory activity against LPS primed mouse J774.A1 cells assessed suppression of LPS/ATP induced IL-beta release preincubated for 30 mins followed by ATP stimulation measured after 30 mins by ELISA
Antiinflammatory activity against LPS primed mouse J774.A1 cells assessed suppression of LPS/ATP induced IL-beta release preincubated for 30 mins followed by ATP stimulation measured after 30 mins by ELISA
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[PMID: 36073117] |
HDAC6-IN-13 (Compound 35m) (0.1-1 μM; 24 h) is highly selective toward HDAC6 versus class I HDACs[1].
HDAC6-IN-13 is a slow-on and slow-off tight-binding HDAC6 inhibitor, while exhibits fast-on properties for HDAC1, 2, and 3[1].
HDAC6-IN-13 (5-20 μM; 8 h) shows anti-inflammatory activity in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4−11 and J774A.1
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Concentration:0.1, 0.2, 0.5 and 1 μM
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Incubation Time:24 h
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Result:Concentration-related accumulation of acetylated tubulin (Ac-Tubulin) was observed, while upregulation of acetylated histone H3 (AcHH3) and acetylated histone H4 (AcHH4) was not apparent even at the concentration of 1 μM.
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Cell Line:J774A.1 cells
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Concentration:5, 10 and 20 μM
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Incubation Time:8 h
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Result:Inhibited the cleavage of pro-caspase 1 to p20 in a dose-dependent manner, inhibited the interaction between HDAC6 and dynein.
HDAC6-IN-13 (20 mg/kg; p.o.; once) shows very high oral bioavailability (F% = 93.4%) and significant BBB permeability in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 WT mice, LPS-induced endotoxic shock model[1]
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Dosage:20 mg/kg
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Administration:PO and IP, immediately after the LPS injection
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Result:Significantly decreased the serum IL-1β levels in LPS-induced mice via both ip and po administration.
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Animal Model:Male CD-1 mice[1]
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Dosage:5 mg/kg or 20 mg/kg
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Administration:IV (5 mg/kg) or PO (20 mg/kg) (Pharmacokinetic Study)
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Result:Pharmacokinetics Characterization of HDAC6-IN-13 (Compound 35m) with iv and Oral Administrationa[1]
PK parameters HDAC6-IN-13 HDAC6-IN-13 administered dose (mg/kg) iv at 5 mg/kg oral at 20 mg/kg Cmax (ng/mL) 4604 ± 551 5570 ± 551 t1/2 (h) 7.95 ± 0.370 6.80 ± 0.145 AUC0−inf (ng•h/mL) 2755 ± 395 10292 ± 1385 F% n/a 93.4 ± 12.6
aHDAC6-IN-13 was administrated via iv and po (n = 3). The blood sample was collected at different time points after dosing, and the plasma concentration of HDAC6-IN-13 was determined via LC-MS/MS. The area under the plasma concentration versus time curve (AUC) was calculated using the linear trapezoidal method. The pharmacokinetic parameters were obtained using the noncompartmental method. Data are shown as mean ± SD.
化学情報
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CAS 番号 2837128-41-1
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性状 Solid
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分子量 370.45
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分子式 C23H22N4O
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Color Light yellow to yellow
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SMILES
CCNNC(C1=CC=C(C=C1)CN2C3=CC=CC=C3C=CC4=C2C=NC=C4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (337.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (281 KB)
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SDS (251 KB)
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- Français - FR (251 KB)
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- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6994 mL | 13.4971 mL | 26.9942 mL | 67.4855 mL |
| 5 mM | 0.5399 mL | 2.6994 mL | 5.3988 mL | 13.4971 mL | |
| 10 mM | 0.2699 mL | 1.3497 mL | 2.6994 mL | 6.7485 mL | |
| 15 mM | 0.1800 mL | 0.8998 mL | 1.7996 mL | 4.4990 mL | |
| 20 mM | 0.1350 mL | 0.6749 mL | 1.3497 mL | 3.3743 mL | |
| 25 mM | 0.1080 mL | 0.5399 mL | 1.0798 mL | 2.6994 mL | |
| 30 mM | 0.0900 mL | 0.4499 mL | 0.8998 mL | 2.2495 mL | |
| 40 mM | 0.0675 mL | 0.3374 mL | 0.6749 mL | 1.6871 mL | |
| 50 mM | 0.0540 mL | 0.2699 mL | 0.5399 mL | 1.3497 mL | |
| 60 mM | 0.0450 mL | 0.2250 mL | 0.4499 mL | 1.1248 mL | |
| 80 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.8436 mL | |
| 100 mM | 0.0270 mL | 0.1350 mL | 0.2699 mL | 0.6749 mL |
HDAC6-IN-13 関連分類
HY-151261 関連分類
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