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Purity: ≥98%
ML329 is a potent small molecule inhibitor of MITF (Micropthalmia-associated transcription factor) which inhibits TRPM-1 (melastatin, a MITF target gene) promoter activity with an IC50 of 1.2 μM. MITF is a lineage restricted basic helix-loop-helix leucine zipper transcription factor that is essential for melanocyte development, function and survival. 15% of human melanomas have MITF gene amplification. In addition, a vast majority of melanomas are dependent upon MITF for survival. ML329 was discovered by a high throughput screening (HTS) of 331,578 compounds from the NIH MLPCN compound library. ML329 was tested in two MITF-dependent melanoma cell viability assays, SK-MEL-5 and MALME-3M plus a MITF-independent cell line, A375. ML329 showed specific activity against the MITF-dependent cells, primary melanocytes but no effect on the viability in A375 cells. ML329 reduced the expression of multiple MITF target genes, including pigment-related genes and the cell cycle regulator CDK2. As a tool compound, ML329 will be useful in elucidating the role of MITF in melanocyte lineage development and in melanoma disease progression.
| ln Vitro |
Many target genes of the micropthalmia-associated transcription factor (MITF) are inhibited by ML329, which also prevents the growth of many cell lines that depend on MITF. MITF or other elements of the MITF regulatory network may come into contact with ML329 directly or indirectly. Since MITF is a transcription factor that controls pigmentation and the cell cycle, interfering with ML329 will help identify the precise functions of MITF in melanoma and confirm that blocking MITF function may be a viable melanoma treatment. While ML329 has no effect on the viability of A375 cells, it exhibits particular activity against primary melanocytes that are dependent on MITF. ML329 inhibits the expression of several MITF target genes, including as genes associated to pigmentation and CDK2, a regulator of the cell cycle. As a tool chemical, ML329 will be helpful in clarifying how MITF functions in the establishment of melanocyte lineages and in the advancement of melanoma disease[1].
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| References |
[1]. Faloon PW, et al. A Small Molecule Inhibitor of the MITF Molecular Pathway. Probe Reports from the NIH Molecular Libraries Program . Bethesda (MD): National Center for Biotechnology Information (US); 2010-2012 Dec 13.
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| Molecular Formula |
C₁₆H₁₂N₂O₄S
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| Molecular Weight |
328.34
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| CAS # |
19992-50-8
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| SMILES |
O=S(C1=CC=C(NC(C2=O)=CC(C3=C2C=CC=C3)=O)C=C1)(N)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (15.23 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0456 mL | 15.2281 mL | 30.4562 mL | |
| 5 mM | 0.6091 mL | 3.0456 mL | 6.0912 mL | |
| 10 mM | 0.3046 mL | 1.5228 mL | 3.0456 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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