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| 5mg |
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Purity: ≥98%
NSC 185058 (NSC-185058) is an inhibitor of ATG4B which is a major cysteine protease, and inhibition of ATG4B by NSC185058 markedly attenuates autophagic activity. NSC185058 acts by inhibiting autophagy and showing a negative impact on osteosarcoma tumors.
| ln Vivo |
An antagonist of ATG4B is NSC185058. By reversibly altering ATG8 to encourage autophagosomes, ATG4B promotes autophagy. Radiation therapy (RT) has an enhanced antitumor activity when it contains ATG4B-conjugated NSC185058. NSC185058 was found to decrease the tumorigenicity of astroblastoma (GBM) cells and increase the antitumor activity of RT in an orthotopic GBM xenograft model [1].
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| References |
[1]. Huang T, et al. MST4 Phosphorylation of ATG4B Regulates Autophagic Activity, Tumorigenicity, and Radioresistance in Glioblastoma. Cancer Cell. 2017 Dec 11;32(6):840-855.e8.
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| Molecular Formula |
C11H9N3S
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|---|---|
| Molecular Weight |
215.27426
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| CAS # |
39122-38-8
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| SMILES |
S=C(C1=NC=CC=C1)NC2=NC=CC=C2
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| InChi Key |
UGWOJXZJIZUKDP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H9N3S/c15-11(9-5-1-3-7-12-9)14-10-6-2-4-8-13-10/h1-8H,(H,13,14,15)
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| Chemical Name |
N-Pyridin-2-ylpyridine-2-carbothioamide
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| Synonyms |
NSC185058; NSC-185058; NSC 185058;
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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 : ≥ 125 mg/mL (~580.67 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (9.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (9.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6453 mL | 23.2266 mL | 46.4533 mL | |
| 5 mM | 0.9291 mL | 4.6453 mL | 9.2907 mL | |
| 10 mM | 0.4645 mL | 2.3227 mL | 4.6453 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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