Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
HDAC1 0.098 μM (IC50) HDAC2 0.156 μM (IC50) HDAC3 0.039 μM (IC50) HDAC6 0.015 μM (IC50) HDAC8 0.047 μM (IC50) HDAC10 0.071 μM (IC50) HDAC4 2.73 μM (IC50) HDAC5 1.35 μM (IC50) HDAC7 2.06 μM (IC50) HDAC9 2.79 μM (IC50) HDAC11 3.98 μM (IC50)
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ln Vitro |
Compound 5e, MC2625, has a 72-hour half-life of 0.07 μM for colorectal cancer cells, 0.32 μM for lung adenocarcinoma cells, and 0.05 μM for chronic myelogenous leukemia cells [1]. The G2/M cell cycle arrest is induced by MC2625 (1, 5 μM; 24, 48 hours) [1]. Acetyl-α-tubulin levels rise, H3K9/14 hyperacetylation activity is induced, and p21 protein is dramatically upregulated by MC2625 (1, 5 μM; 24, 48 hours) [1]. Inducing apoptosis, MC2625 (1, 5 μM; 48 hours) downregulates cyclin D1 and BCL-2, enhances the mRNA expression of p21, BAX, and BAK, and modifies pro- and anti-apoptotic microRNA [1].
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Cell Assay |
Cell Cycle Analysis[1]
Cell Types: Human acute myeloid leukaemia U937 cells Tested Concentrations: 1, 5 μM Incubation Duration: 24, 48 h Experimental Results: At 24 h, demonstrated very low increase of the pre-G1 peak and led to a G2/M phase arrest at 1 μM; induced a 10% pre-G1 increase and displayed a block at the G2/M phase at 5 μM. At 48 h, induced a 70-85% block of the cell cycle at the G1 phase. Western Blot Analysis[1] Cell Types: Human acute myeloid leukaemia U937 cells Tested Concentrations: 1, 5 μM Incubation Duration: 24, 48 h Experimental Results: At 1 μM revealed H3K9/14 hyperacetylation activity, increased the acetyl-α-tubulin level, markedly upregulated the p21 protein. RT-PCR[1] Cell Types: Human acute myeloid leukaemia U937 cells Tested Concentrations: 1, 5 μM Incubation Duration: 48 h Experimental Results: At 1 μM Dramatically induced the expression of BAX and BAK, dose-dependently downregulated the antiapoptotic factor BCL-2. Downregulated miRNAs with antiapoptotic activity (miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p,miR-21-5p); induced the proapoptotic miRNAs (miR-let7a-5p, miR-125b-5p, miR-181a-5p, miR-181b-5p, miR-769-5p, miR-122-5p). |
References |
[1]. Elisabetta Di Bello, et al. Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells. Eur J Med Chem. 2022 Dec 15;247:115022.
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Molecular Formula |
C20H17N3O3
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Molecular Weight |
347.37
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CAS # |
2284460-01-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1(CC(NC2=CC=C(C=CC(NO)=O)N=C2)=O)=C2C(C=CC=C2)=CC=C1
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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.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8788 mL | 14.3939 mL | 28.7877 mL | |
5 mM | 0.5758 mL | 2.8788 mL | 5.7575 mL | |
10 mM | 0.2879 mL | 1.4394 mL | 2.8788 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.