ML329
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MedKoo CAT#: 555752

CAS#: 19992-50-8

Description: ML-329 is an inhibitor of the microphthalmia-associated transcription factor (MITF) pathway with an IC50 value of 1.2 μM for promoter activity of the MITF target gene TRPM-1. 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.

Chemical Structure

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ML329
CAS# 19992-50-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555752
Name: ML329
CAS#: 19992-50-8
Chemical Formula: C16H12N2O4S
Exact Mass: 328.05
Molecular Weight: 328.342
Elemental Analysis: C, 58.53; H, 3.68; N, 8.53; O, 19.49; S, 9.76

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 2650 2 Weeks
1g USD 3850 2 Weeks
2g USD 6450 2 Weeks
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Synonym: ML329; ML 329; ML-329; CID 12387471; CID12387471; CID-12387471;

IUPAC/Chemical Name: 4-[(1,4-dihydro-1,4-dioxo-2-naphthalenyl)amino]-benzenesulfonamide

InChi Key: CSYFFQVEQXEIAB-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H12N2O4S/c17-23(21,22)11-7-5-10(6-8-11)18-14-9-15(19)12-3-1-2-4-13(12)16(14)20/h1-9,18H,(H2,17,21,22)

SMILES Code: O=S(C1=CC=C(NC(C2=O)=CC(C3=C2C=CC=C3)=O)C=C1)(N)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Micropthalmia-associated transcription factor (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.

Product Data:
Product Data
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Biological target: ML329 is a micropthalmia-associated transcription factor (MITF) inhibitor, which inhibits TRPM-1 promoter activity with an IC50 of 1.2 μM.
In vitro activity: 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. Reference: Probe Reports from the NIH Molecular Libraries Program [Internet]. 2012 Dec 13 [updated 2014 Sep 18]. https://pubmed.ncbi.nlm.nih.gov/24027801/
In vivo activity: The effect of potential probiotics derived from breast milk on development of intrauterine growth retardation (IUGR) newborn rats' intestine was investigated. The proliferation and differentiation stimulating effects of ML-329 and ML-446 on IECs in the jejunum, ileum, and colon were mediated by activating the Wnt pathway with increased expression of wnt, lrp5, and β-catenin genes and accumulation of β-catenin, and by downregulating the Notch signalling pathway with decreased expression of the activated notch protein. Reference: J Appl Microbiol. 2022 Aug;133(2):503-514. https://pubmed.ncbi.nlm.nih.gov/35429125/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 12.5 38.07
DMSO 30.3 92.38
DMSO:PBS (pH 7.2) (1:1) 0.5 1.52
Ethanol 0.1 0.30

Preparing Stock Solutions

The following data is based on the product molecular weight 328.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Proaño-Pérez E, Ollé L, Guo Y, Aparicio C, Guerrero M, Muñoz-Cano R, Martin M. MITF Downregulation Induces Death in Human Mast Cell Leukemia Cells and Impairs IgE-Dependent Degranulation. Int J Mol Sci. 2023 Feb 9;24(4):3515. doi: 10.3390/ijms24043515. PMID: 36834926; PMCID: PMC9961600. 2. Faloon PW, Bennion M, Weiner WS, Smith RA, Wurst J, Weiwer M, Hartland C, Mosher CM, Johnston S, Porubsky P, Neuenswander B, Dandapani S, Munoz B, Schoenen FJ, Metkar S, Haq R, Fisher DE, Aubé J, Palmer M, Schreiber SL. A Small Molecule Inhibitor of the MITF Molecular Pathway. 2012 Dec 13 [updated 2014 Sep 18]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. PMID: 24027801. 3. Lyu L, Zhou X, Zhang M, Liu L, Liu T, Niu H, Wu Y, Liang C, Han X, Zhang L. Lactobacillus derived from breast milk facilitates intestinal development in IUGR rats. J Appl Microbiol. 2022 Aug;133(2):503-514. doi: 10.1111/jam.15576. Epub 2022 Apr 27. PMID: 35429125.
In vitro protocol: 1. Proaño-Pérez E, Ollé L, Guo Y, Aparicio C, Guerrero M, Muñoz-Cano R, Martin M. MITF Downregulation Induces Death in Human Mast Cell Leukemia Cells and Impairs IgE-Dependent Degranulation. Int J Mol Sci. 2023 Feb 9;24(4):3515. doi: 10.3390/ijms24043515. PMID: 36834926; PMCID: PMC9961600. 2. Faloon PW, Bennion M, Weiner WS, Smith RA, Wurst J, Weiwer M, Hartland C, Mosher CM, Johnston S, Porubsky P, Neuenswander B, Dandapani S, Munoz B, Schoenen FJ, Metkar S, Haq R, Fisher DE, Aubé J, Palmer M, Schreiber SL. A Small Molecule Inhibitor of the MITF Molecular Pathway. 2012 Dec 13 [updated 2014 Sep 18]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. PMID: 24027801.
In vivo protocol: 1. Lyu L, Zhou X, Zhang M, Liu L, Liu T, Niu H, Wu Y, Liang C, Han X, Zhang L. Lactobacillus derived from breast milk facilitates intestinal development in IUGR rats. J Appl Microbiol. 2022 Aug;133(2):503-514. doi: 10.1111/jam.15576. Epub 2022 Apr 27. PMID: 35429125.

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Faloon PW, Bennion M, Weiner WS, et al. A Small Molecule Inhibitor of the MITF Molecular Pathway. In: Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD): National Center for Biotechnology Information (US); 2010.