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MedKoo Cat#: 562101 | Name: NSC185058
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Description:

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

NSC185058 is an ATG4B antagonist. It acts by inhibiting autophagy and showing a negative impact on osteosarcoma tumors.

Chemical Structure

NSC185058
NSC185058
CAS#39122-38-8

Theoretical Analysis

MedKoo Cat#: 562101

Name: NSC185058

CAS#: 39122-38-8

Chemical Formula: C11H9N3S

Exact Mass: 215.0517

Molecular Weight: 215.27

Elemental Analysis: C, 61.37; H, 4.21; N, 19.52; S, 14.89

Price and Availability

Size Price Availability Quantity
1g USD 2,950.00 2-3 months
2g USD 5,450.00 2-3 months
5g USD 7,450.00 2-3 months
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Related CAS #
No Data
Synonym
NSC185058; NSC-185058; NSC 185058;
IUPAC/Chemical Name
N-Pyridin-2-ylpyridine-2-carbothioamide
InChi Key
UGWOJXZJIZUKDP-UHFFFAOYSA-N
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)
SMILES Code
S=C(C1=NC=CC=C1)NC2=NC=CC=C2
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:
NSC 185058 is an inhibitor of ATG4B, a major cysteine protease.
In vitro activity:
NSC185058 inhibited the C-terminal cleavage of LC3B by ATG4B in rapamycin-treated 293T cells and in amino acid starved HuH7 cells. Meanwhile, NSC377071 had a minimal effect on rapamycin-induced ATG4B activity in 293T cells as evidenced by LC3B cleavage, but inhibited starvation-induced activity in HuH7 cells. The results demonstrate that NSC185058 effectively inhibits ATG4B activity in vitro and in cells, but that NSC377071 is likely acting on a different target protein. NSC185058 was found to be cytotoxic to Saos-2 cells during a 48 h exposure (Fig. 8A). Reference: Autophagy. 2014;10(11):2021-35. https://pubmed.ncbi.nlm.nih.gov/25483883/
In vivo activity:
In vivo, NSC (NSC185058) and CQ significantly decreased M83 glioma xenograft growth in the flanks of mice (Figures S7C–S7E). NSC did not enhance the effects of STK26 knockout (KO) on M83 xenograft growth and autophagic activity in vivo (Figures S7F–S7I). Reference: Cancer Cell. 2017 Dec 11;32(6):840-855.e8. https://pubmed.ncbi.nlm.nih.gov/29232556/
Solvent mg/mL mM
Solubility
DMF 30.0 139.36
DMSO 66.0 306.59
Ethanol 11.8 54.58
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 215.27 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. Hiura F, Kawabata Y, Aoki T, Mizokami A, Jimi E. Inhibition of the ATG4-LC3 pathway suppressed osteoclast maturation. Biochem Biophys Res Commun. 2022 Dec 3;632:40-47. doi: 10.1016/j.bbrc.2022.09.065. Epub 2022 Sep 20. PMID: 36198202. 2. Akin D, Wang SK, Habibzadegah-Tari P, Law B, Ostrov D, Li M, Yin XM, Kim JS, Horenstein N, Dunn WA Jr. A novel ATG4B antagonist inhibits autophagy and has a negative impact on osteosarcoma tumors. Autophagy. 2014;10(11):2021-35. doi: 10.4161/auto.32229. Epub 2014 Oct 30. PMID: 25483883; PMCID: PMC4502682. 3. Rosa-Caldwell ME, Jansen LT, Lim S, Dunlap KR, Haynie WS, Washington TA, Greene NP. Neither autophagy nor exercise training mode affect exercise-induced beneficial adaptations in high fat-fed mice. Sports Med Health Sci. 2020 Mar 9;2(1):44-53. doi: 10.1016/j.smhs.2020.03.003. PMID: 35783331; PMCID: PMC9219353. 4. Huang T, Kim CK, Alvarez AA, Pangeni RP, Wan X, Song X, Shi T, Yang Y, Sastry N, Horbinski CM, Lu S, Stupp R, Kessler JA, Nishikawa R, Nakano I, Sulman EP, Lu X, James CD, Yin XM, Hu B, Cheng SY. MST4 Phosphorylation of ATG4B Regulates Autophagic Activity, Tumorigenicity, and Radioresistance in Glioblastoma. Cancer Cell. 2017 Dec 11;32(6):840-855.e8. doi: 10.1016/j.ccell.2017.11.005. PMID: 29232556; PMCID: PMC5734934.
In vitro protocol:
1. Hiura F, Kawabata Y, Aoki T, Mizokami A, Jimi E. Inhibition of the ATG4-LC3 pathway suppressed osteoclast maturation. Biochem Biophys Res Commun. 2022 Dec 3;632:40-47. doi: 10.1016/j.bbrc.2022.09.065. Epub 2022 Sep 20. PMID: 36198202. 2. Akin D, Wang SK, Habibzadegah-Tari P, Law B, Ostrov D, Li M, Yin XM, Kim JS, Horenstein N, Dunn WA Jr. A novel ATG4B antagonist inhibits autophagy and has a negative impact on osteosarcoma tumors. Autophagy. 2014;10(11):2021-35. doi: 10.4161/auto.32229. Epub 2014 Oct 30. PMID: 25483883; PMCID: PMC4502682.
In vivo protocol:
1. Rosa-Caldwell ME, Jansen LT, Lim S, Dunlap KR, Haynie WS, Washington TA, Greene NP. Neither autophagy nor exercise training mode affect exercise-induced beneficial adaptations in high fat-fed mice. Sports Med Health Sci. 2020 Mar 9;2(1):44-53. doi: 10.1016/j.smhs.2020.03.003. PMID: 35783331; PMCID: PMC9219353. 2. Huang T, Kim CK, Alvarez AA, Pangeni RP, Wan X, Song X, Shi T, Yang Y, Sastry N, Horbinski CM, Lu S, Stupp R, Kessler JA, Nishikawa R, Nakano I, Sulman EP, Lu X, James CD, Yin XM, Hu B, Cheng SY. MST4 Phosphorylation of ATG4B Regulates Autophagic Activity, Tumorigenicity, and Radioresistance in Glioblastoma. Cancer Cell. 2017 Dec 11;32(6):840-855.e8. doi: 10.1016/j.ccell.2017.11.005. PMID: 29232556; PMCID: PMC5734934.
1: Huang T, Kim CK, Alvarez AA, Pangeni RP, Wan X, Song X, Shi T, Yang Y, Sastry N, Horbinski CM, Lu S, Stupp R, Kessler JA, Nishikawa R, Nakano I, Sulman EP, Lu X, James CD, Yin XM, Hu B, Cheng SY. MST4 Phosphorylation of ATG4B Regulates Autophagic Activity, Tumorigenicity, and Radioresistance in Glioblastoma. Cancer Cell. 2017 Dec 11;32(6):840-855.e8. doi: 10.1016/j.ccell.2017.11.005. PubMed PMID: 29232556; PubMed Central PMCID: PMC5734934. 2: Akin D, Wang SK, Habibzadegah-Tari P, Law B, Ostrov D, Li M, Yin XM, Kim JS, Horenstein N, Dunn WA Jr. A novel ATG4B antagonist inhibits autophagy and has a negative impact on osteosarcoma tumors. Autophagy. 2014;10(11):2021-35. doi: 10.4161/auto.32229. Epub 2014 Oct 30. PubMed PMID: 25483883; PubMed Central PMCID: PMC4502682.

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VS-II-173