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| 5mg |
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| 25mg |
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Purity: ≥98%
| Targets |
AZ-33 targets lactate dehydrogenase A (LDHA), the key enzyme involved in anaerobic glycolysis. LDHA catalyzes the conversion of pyruvate to lactate, regenerating NAD+ in the process. This enzyme is frequently deregulated in human malignancies, making it a potential target for cancer therapy. AZ-33 is a selective inhibitor of LDHA, with an IC50 of 0.5 μM. It binds to LDHA with a Kd of 0.093 μM. It is selective for LDHA over LDHB in an NADH competition assay using recombinant enzymes (IC50s = 0.54 and 3.6 μM, respectively).
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| ln Vitro |
In vitro, AZ-33 inhibits LDHA activity with an IC50 of 0.5 μM. It binds to human LDHA with a Kd of 0.093 μM. AZ-33 is cell-impermeable and lacks cytotoxicity against HeLa cervical cancer cells (IC50 > 500 μM). Its selectivity for LDHA over LDHB has been demonstrated in enzyme assays. By inhibiting LDHA, AZ-33 disrupts the metabolic activity of cancer cells and has the potential to impair their growth and survival.
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| ln Vivo |
Specific in vivo data for AZ-33 are not detailed in the available literature. However, as an LDHA inhibitor, it may have therapeutic applications in the treatment of cancer by targeting the altered metabolism of cancer cells. Its cell-impermeability suggests that its in vivo effects would be limited to extracellular or non-cell-autonomous mechanisms.
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| Enzyme Assay |
The enzymatic activity of AZ-33 can be assessed using LDHA enzyme assays. Recombinant human LDHA is incubated with its substrate, pyruvate, and NADH in the presence of varying concentrations of the inhibitor. The conversion of NADH to NAD+ is measured spectrophotometrically by monitoring the decrease in absorbance at 340 nm. The IC50 value for LDHA inhibition is determined from dose-response curves. The binding affinity (Kd) can be measured using surface plasmon resonance (SPR).
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| Cell Assay |
To evaluate the cellular effects of AZ-33, cells are treated with the compound, and the levels of lactate and other metabolites are measured. The effects on cell proliferation and survival are assessed using standard assays. However, AZ-33 is cell-impermeable and lacks cytotoxicity against HeLa cells (IC50 > 500 μM), suggesting that it may not be suitable for direct cellular studies.
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| Animal Protocol |
In vivo studies with AZ-33 would typically involve administration to tumor-bearing mice. The compound's effects on tumor growth, lactate levels, and other metabolic parameters would be measured. However, its cell-impermeability may limit its utility in vivo.
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| ADME/Pharmacokinetics |
AZ-33 has a molecular formula of C25H27N3O6S and a molecular weight of 497.56. Its CAS number is 1370290-34-8. The compound is soluble in DMF (30 mg/mL) and DMSO (30 mg/mL), and slightly soluble in ethanol and PBS. It should be stored at -20°C. The purity is ≥95%.
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| Toxicity/Toxicokinetics |
Specific toxicology data for AZ-33 are not detailed in the available literature. However, it lacks cytotoxicity against HeLa cervical cancer cells (IC50 > 500 μM), suggesting a potentially low toxicity profile. As with all research compounds, standard safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
AZ-33 (LDHA Inhibitor 33) is a potent inhibitor of lactate dehydrogenase A (LDHA) used in cancer research. By targeting the altered metabolism of cancer cells, AZ-33 may have therapeutic applications in the treatment of cancer. It is a valuable tool for studying the role of LDHA in cancer metabolism. It is not a clinically approved drug.
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| Molecular Formula |
C25H27N3O6S
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|---|---|
| Molecular Weight |
497.566
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| Exact Mass |
497.162
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| CAS # |
1370290-34-8
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| Related CAS # |
1370290-34-8;
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| PubChem CID |
56844254
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
843.9±65.0 °C at 760 mmHg
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| Flash Point |
464.2±34.3 °C
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| Vapour Pressure |
0.0±3.3 mmHg at 25°C
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| Index of Refraction |
1.659
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
35
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| Complexity |
744
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SGFJAJFBGVAOFW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H27N3O6S/c1-15-27-20-10-9-18(14-21(20)35-15)28-23(30)11-12-26-22(29)4-2-3-16-5-7-17(8-6-16)13-19(24(31)32)25(33)34/h5-10,14,19H,2-4,11-13H2,1H3,(H,26,29)(H,28,30)(H,31,32)(H,33,34)
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| Chemical Name |
2-(4-(4-((3-((2-Methylbenzo[d]thiazol-6-yl)amino)-3-oxopropyl)amino)-4-oxobutyl)benzyl)malonic acid
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| Synonyms |
AZ-33 AZ 33 AZ33 LDHA Inhibitor 33.
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~100 mg/mL (~200.98 mM)
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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 | 2.0098 mL | 10.0488 mL | 20.0977 mL | |
| 5 mM | 0.4020 mL | 2.0098 mL | 4.0195 mL | |
| 10 mM | 0.2010 mL | 1.0049 mL | 2.0098 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.
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