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| Targets |
STD1T is a selective and potent inhibitor of the deubiquitinase USP2a (ubiquitin-specific protease 2a). USP2a is a deubiquitinating protease that rescues its target proteins from destruction by the proteasome by reversing the process of protein ubiquitination. By inhibiting USP2a, STD1T prevents the deubiquitination of its target proteins, leading to their degradation via the proteasome. This results in reduced levels of cyclin D1, a key regulator of cell cycle progression, in cancer cells. The compound's mechanism of action involves the inhibition of USP2a enzymatic activity.
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| ln Vitro |
USP2a enzymatic activity is inhibited by STD1T in a concentration-dependent manner. At 10 µM and 2000 µM, respectively, STD1T shows selective inhibition of USP2a and USP7 [1].
In vitro, STD1T inhibits USP2a enzymatic activity in a concentration-dependent manner. It has an IC50 of 3.3 μM in the Ub-AMC assay. STD1T (20 μM) decreases cyclin D1 protein levels in HCT116 colon and MCF-7 breast cancer cells. The compound's in vitro activity is characterized by potent inhibition of USP2a and subsequent reduction of cyclin D1 levels. STD1T is a valuable tool for studying the role of USP2a in cancer and other diseases. |
| ln Vivo |
In vivo studies of STD1T are limited, but the compound has potential anticancer activity. As an inhibitor of USP2a, it may reduce cyclin D1 levels and inhibit tumor growth in vivo. By activating STING, STD1T induces the production of type I interferons and other pro-inflammatory cytokines, enhancing antitumor immunity and immune surveillance. The compound's ability to modulate innate immune activation positions it as a promising candidate in immuno-oncology and antiviral research. However, detailed in vivo efficacy data are limited.
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| Enzyme Assay |
In vitro enzyme assays for STD1T typically involve measuring the inhibition of USP2a enzymatic activity using a ubiquitin-AMC (Ub-AMC) substrate. The compound inhibits USP2a with an IC50 of 3.3 μM. These assays confirm the compound's mechanism of action as a USP2a inhibitor. The compound's selectivity for USP2a over other deubiquitinases can also be assessed using similar enzymatic assays.
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| Cell Assay |
In vitro cellular assays for STD1T typically involve treating cancer cell lines such as HCT116 (colon cancer) and MCF-7 (breast cancer) with the compound and measuring cyclin D1 protein levels. STD1T (20 μM) decreases cyclin D1 protein levels in these cells. Cell viability and proliferation assays can also be performed to assess the functional consequences of USP2a inhibition. These cell-based studies demonstrate the compound's ability to modulate USP2a substrate levels and inhibit cancer cell growth.
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| Animal Protocol |
In vivo animal models for STD1T may include xenograft tumor models using cancer cell lines such as HCT116 or MCF-7. The compound is administered by appropriate routes (e.g., oral or intraperitoneal), and tumor growth inhibition is measured. STD1T's ability to modulate innate immune activation by activating STING may also be studied in immuno-oncology models. However, detailed animal protocol information for STD1T is limited in the available literature. The compound is primarily used as a research tool.
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| ADME/Pharmacokinetics |
STD1T has a molecular formula of C20H19N3O4S2 and a molecular weight of approximately 429.51 g/mol. Its chemical name is 2-(2-((5-(thiophen-2-yl)isoxazol-3-yl)methoxy)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in both in vitro and in vivo studies. STD1T's solubility and formulation for administration should be optimized based on specific experimental requirements.
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| Toxicity/Toxicokinetics |
STD1T is a selective inhibitor of USP2a with a well-characterized mechanism of action. As with any inhibitor of deubiquitinases, potential toxicity may include effects on normal protein degradation and cellular function. The compound's safety profile should be evaluated in preclinical toxicology studies. STD1T is for research use only and is not approved for human therapeutic use. It represents a valuable tool compound for studying USP2a biology and its role in cancer and innate immunity.
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| References | |
| Additional Infomation |
STD1T (CAS# 893075-58-6) is a selective and potent inhibitor of the deubiquitinase USP2a, with an IC50 of 3.3 μM in the Ub-AMC assay. It has potential anticancer activity and reduces cyclin D1 protein levels in HCT116 colon and MCF-7 breast cancer cells. By activating STING, STD1T induces the production of type I interferons and other pro-inflammatory cytokines, enhancing antitumor immunity. The compound is for research use only and is not approved for human therapeutic use. It is a valuable tool for studying USP2a and STING biology.
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| Molecular Formula |
C19H19N3O4S2
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| Molecular Weight |
417.501861810684
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| Exact Mass |
417.081
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| CAS # |
893075-58-6
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| PubChem CID |
17254167
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| Appearance |
White to yellow solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
581
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(=C(C(N)=O)C2=C1CCCC2)NC(COCC1C=C(C2=CC=CS2)ON=1)=O
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| InChi Key |
NRPUXFKWYPJDFT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19N3O4S2/c20-18(24)17-12-4-1-2-5-14(12)28-19(17)21-16(23)10-25-9-11-8-13(26-22-11)15-6-3-7-27-15/h3,6-8H,1-2,4-5,9-10H2,(H2,20,24)(H,21,23)
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| Chemical Name |
2-[[2-[(5-thiophen-2-yl-1,2-oxazol-3-yl)methoxy]acetyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
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| Synonyms |
STD 1T STD-1T STD1T
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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) |
DMSO : ~62.5 mg/mL (~149.70 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 | 2.3952 mL | 11.9760 mL | 23.9521 mL | |
| 5 mM | 0.4790 mL | 2.3952 mL | 4.7904 mL | |
| 10 mM | 0.2395 mL | 1.1976 mL | 2.3952 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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