| ln Vitro |
HDAC1/6-IN-3 (compound 15a) (72 h) showed excellent inhibitory activity against HepG2 (IC50 = 0.12 μM), PC9 (IC50 = 0.53 μM), HCT116 (IC50 = 1.12 μM) and MCF7 cells (IC50 = 3.12 μM) [1]. HDAC1/6-IN-3 (0.2–0.5 μM, 24 h) dose-dependently increased the levels of acetylated H3 and H4 in HepG2 cells [1]. HDAC1/6-IN-3 (0.2–0.5 μM, 10–14 days) dose-dependently inhibited colony formation in HepG2 cells [1]. HDAC1/6-IN-3 (0.2-0.5 μM, 24 h) induces G0/G1 phase arrest in HepG2 cells, which may be related to the downregulation of CDK4 and Cyclin D1 proteins [1]. HDAC1/6-IN-3 (0.2-0.5 μM, 48 h) enhances ROS generation and DNA damage accumulation, thereby inducing apoptosis in HepG2 cells [1]. HDAC1/6-IN-3 (0.2-0.5 μM, 24-48 h) triggers pyroptosis in HepG2 cells by cleaving GSDME with caspase-3 [1].
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| ln Vivo |
HDAC1/6-IN-3 (compound 15a) (10 mg/kg, intraperitoneal injection, twice a week for 3 weeks) showed significant antitumor efficacy and acceptable safety in the HepG2 xenograft model [1].
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| Cell Assay |
Cell cycle analysis [1]
Cell Types: HepG2 cells Tested Concentrations: 0.2 and 0.5 μM Incubation Duration: 24 hours Experimental Results: The G0/G1 phase of HepG2 cells was significantly inhibited in a dose-dependent manner. The proportion of G2/M phase decreased from 25.34% to 22.85%, and the proportion of S phase decreased from 32.99% to 13.72%. Apoptosis analysis [1] Cell Types: HepG2 cells Tested Concentrations: 0.2 and 0.5 μM Incubation Duration: 48 hours Experimental Results: 28.2% apoptosis was induced at 0.2 µM and 46.5% at 0.5 µM. Immunofluorescence [1] Cell Types: HepG2 cells Tested Concentrations: 0.2 and 0.5 μM Incubation Duration: 24 hours Experimental Results: Dose-dependent increase in ROS levels. Dose-dependent formation of γH2AX foci was observed.
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| Animal Protocol |
Animal/Disease Models:A HepG2-induced xenograft model was established in male BALB/c nude mice [1].
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection (ip), twice weekly for 3 weeks. Experimental Results: Tumor growth was inhibited in a dose-dependent manner. A dose-dependent decrease in Ki67 immunostaining was observed. Increases in Ac-H3/H4, Cl-caspase3, and GSDME-N were induced in a dose-dependent manner. |
| References |
| CAS # |
3038691-85-6
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|---|---|
| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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