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MedKoo Cat#: 407457 | Name: ML364
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

ML364 is a small molecule inhibitor of the deubiquitinase USP2 with potential anticancer activity. ML364 has an IC50 of 1.1 μm in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate. Direct binding of ML364 to USP2 was demonstrated using microscale thermophoresis. ML364 induced an increase in cellular cyclin D1 degradation and caused cell cycle arrest as shown in Western blottings and flow cytometry assays utilizing both Mino and HCT116 cancer cell lines.

Chemical Structure

ML364
ML364
CAS#1991986-30-1

Theoretical Analysis

MedKoo Cat#: 407457

Name: ML364

CAS#: 1991986-30-1

Chemical Formula: C24H18F3N3O3S2

Exact Mass: 517.0742

Molecular Weight: 517.54

Elemental Analysis: C, 55.70; H, 3.51; F, 11.01; N, 8.12; O, 9.27; S, 12.39

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,750.00 2 Weeks
2g USD 6,250.00 2 Weeks
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Related CAS #
No Data
Synonym
ML364; ML 364; ML-364.
IUPAC/Chemical Name
2-[(4-Methylphenyl)sulfonylamino]-N-(4-phenyl-1,3-thiazol-2-yl)-4-(trifluoromethyl)benzamide
InChi Key
QZUGMNXETPARLI-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H18F3N3O3S2/c1-15-7-10-18(11-8-15)35(32,33)30-20-13-17(24(25,26)27)9-12-19(20)22(31)29-23-28-21(14-34-23)16-5-3-2-4-6-16/h2-14,30H,1H3,(H,28,29,31)
SMILES Code
O=C(NC1=NC(C2=CC=CC=C2)=CS1)C3=CC=C(C(F)(F)F)C=C3NS(=O)(C4=CC=C(C)C=C4)=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
>2 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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM).
In vitro activity:
Treatment with this dose of ML364 for 5 days caused > 70% decrease in the incorporation of BrdU to the cells; thus, ML364 decreased the proliferation of C2C12 cells (Fig. 7B). On the other hand, treatment with ML364 for 8 h also decreased the intracellular level of ATP to 64.9% of vehicle‐treated cells (Fig. 7C). Moreover, treatment with ML364 markedly decreased the potential of the mitochondrial membrane in C2C12 cells (0.37‐fold difference vs. that of vehicle‐treated cells, P < 0.001; Fig. 7D). Reference: Physiol Rep. 2019 Jul;7(14):e14193. https://pubmed.ncbi.nlm.nih.gov/31353872/
In vivo activity:
In the P. aeruginosa PAO1 or the CRPA 16-2 infection mouse model, ML364 treatment could significantly improve the survival rate from 0% to 70% or from 30% to 90%, respectively. The survival rates of mice infected with S. aureus ATCC 29213 or MRSA 08-50 could be increased from 20% to 50% or even from 10% to 70%, by the administration of ML364 (Figure 5C). In Figure 5D, ML364 was able to significantly reduce the bacterial loads in the organs of mice (p ≤ 0.01), when the mice were systemically infected with CRPA 16-2 or MRSA 08-50. Reference: Front Microbiol. 2022 Dec 22;13:980217. https://pubmed.ncbi.nlm.nih.gov/36619997/
Solvent mg/mL mM comments
Solubility
DMF 30.0 57.97
DMSO 37.7 72.78
DMSO:PBS (pH 7.2) (1:2) 0.3 0.64
Ethanol 22.5 43.47
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 517.54 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. Hashimoto M, Saito N, Ohta H, Yamamoto K, Tashiro A, Nakazawa K, Inanami O, Kitamura H. Inhibition of ubiquitin-specific protease 2 causes accumulation of reactive oxygen species, mitochondria dysfunction, and intracellular ATP decrement in C2C12 myoblasts. Physiol Rep. 2019 Jul;7(14):e14193. doi: 10.14814/phy2.14193. PMID: 31353872; PMCID: PMC6661303. 2. Davis MI, Pragani R, Fox JT, Shen M, Parmar K, Gaudiano EF, Liu L, Tanega C, McGee L, Hall MD, McKnight C, Shinn P, Nelson H, Chattopadhyay D, D'Andrea AD, Auld DS, DeLucas LJ, Li Z, Boxer MB, Simeonov A. Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models. J Biol Chem. 2016 Nov 18;291(47):24628-24640. doi: 10.1074/jbc.M116.738567. Epub 2016 Sep 28. PMID: 27681596; PMCID: PMC5114414. 3. Zhang Y, Dong L, Sun L, Hu X, Wang X, Nie T, Li X, Wang P, Pang P, Pang J, Lu X, Yao K, You X. ML364 exerts the broad-spectrum antivirulence effect by interfering with the bacterial quorum sensing system. Front Microbiol. 2022 Dec 22;13:980217. doi: 10.3389/fmicb.2022.980217. PMID: 36619997; PMCID: PMC9813848. 4. Hashimoto M, Fujimoto M, Konno K, Lee ML, Yamada Y, Yamashita K, Toda C, Tomura M, Watanabe M, Inanami O, Kitamura H. Ubiquitin-Specific Protease 2 in the Ventromedial Hypothalamus Modifies Blood Glucose Levels by Controlling Sympathetic Nervous Activation. J Neurosci. 2022 Jun 8;42(23):4607-4618. doi: 10.1523/JNEUROSCI.2504-21.2022. Epub 2022 May 3. PMID: 35504726; PMCID: PMC9186793.
In vitro protocol:
1. Hashimoto M, Saito N, Ohta H, Yamamoto K, Tashiro A, Nakazawa K, Inanami O, Kitamura H. Inhibition of ubiquitin-specific protease 2 causes accumulation of reactive oxygen species, mitochondria dysfunction, and intracellular ATP decrement in C2C12 myoblasts. Physiol Rep. 2019 Jul;7(14):e14193. doi: 10.14814/phy2.14193. PMID: 31353872; PMCID: PMC6661303. 2. Davis MI, Pragani R, Fox JT, Shen M, Parmar K, Gaudiano EF, Liu L, Tanega C, McGee L, Hall MD, McKnight C, Shinn P, Nelson H, Chattopadhyay D, D'Andrea AD, Auld DS, DeLucas LJ, Li Z, Boxer MB, Simeonov A. Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models. J Biol Chem. 2016 Nov 18;291(47):24628-24640. doi: 10.1074/jbc.M116.738567. Epub 2016 Sep 28. PMID: 27681596; PMCID: PMC5114414.
In vivo protocol:
1. Zhang Y, Dong L, Sun L, Hu X, Wang X, Nie T, Li X, Wang P, Pang P, Pang J, Lu X, Yao K, You X. ML364 exerts the broad-spectrum antivirulence effect by interfering with the bacterial quorum sensing system. Front Microbiol. 2022 Dec 22;13:980217. doi: 10.3389/fmicb.2022.980217. PMID: 36619997; PMCID: PMC9813848. 2. Hashimoto M, Fujimoto M, Konno K, Lee ML, Yamada Y, Yamashita K, Toda C, Tomura M, Watanabe M, Inanami O, Kitamura H. Ubiquitin-Specific Protease 2 in the Ventromedial Hypothalamus Modifies Blood Glucose Levels by Controlling Sympathetic Nervous Activation. J Neurosci. 2022 Jun 8;42(23):4607-4618. doi: 10.1523/JNEUROSCI.2504-21.2022. Epub 2022 May 3. PMID: 35504726; PMCID: PMC9186793.
1: Davis MI, Pragani R, Fox JT, Shen M, Parmar K, Gaudiano EF, Liu L, Tanega C, McGee L, Hall MD, McKnight C, Shinn P, Nelson H, Chattopadhyay D, D'Andrea AD, Auld DS, DeLucas LJ, Li Z, Boxer MB, Simeonov A. Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models. J Biol Chem. 2016 Nov 18;291(47):24628-24640. Epub 2016 Sep 28. PubMed PMID: 27681596; PubMed Central PMCID: PMC5114414.