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.
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- Purity : 98.08%
- CAS No.: 2837128-41-1
- 화학식: C23H22N4O
- 분자량:370.45
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
HDAC6 0.019 μM (IC50) |
HDAC3 1.03 μM (IC50) |
HDAC1 1.53 μM (IC50) |
HDAC2 2.06 μM (IC50) |
Cellular Effect
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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] |
In Vitro
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.
In Vivo
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.
Chemical Information
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CAS No. 2837128-41-1
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Appearance Solid
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분자량 370.45
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 Related Classifications
HY-151261 Related Classifications
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