NSC 319726 | CAT#71555-25-4 | p53R175 reactivator

MedKoo Cat#: 462541 | Name: NSC 319726

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Description:

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

NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.

Chemical Structure

NSC 319726

CAS#71555-25-4

Theoretical Analysis

MedKoo Cat#: 462541

Name: NSC 319726

CAS#: 71555-25-4

Chemical Formula: C11H14N4S

Exact Mass: 234.0939

Molecular Weight: 234.32

Elemental Analysis: C, 56.38; H, 6.02; N, 23.91; S, 13.68

Price and Availability

Size	Price	Availability
5mg	USD 260.00	2 Weeks
10mg	USD 430.00	2 Weeks
25mg	USD 785.00	2 Weeks

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Related CAS #

No Data

Synonym

NSC 319726; NSC-319726; NSC319726

IUPAC/Chemical Name

(E)-N'-(1-(pyridin-2-yl)ethylidene)azetidine-1-carbothiohydrazide

InChi Key

XDHBUMNIQRLHGO-UKTHLTGXSA-N

InChi Code

InChI=1S/C11H14N4S/c1-9(10-5-2-3-6-12-10)13-14-11(16)15-7-4-8-15/h2-3,5-6H,4,7-8H2,1H3,(H,14,16)/b13-9+

SMILES Code

C/C(C1=CC=CC=N1)=N\NC(N2CCC2)=S

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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM).

In vitro activity:

This study investigated the mechanism by which ZMC1 reactivates p53-R175H and provide evidence that ZMC1: 1) restores WT structure by functioning as a zinc-metallochaperone, providing an optimal concentration of zinc to facilitate proper folding; and 2) increases cellular reactive oxygen species that transactivate the newly conformed p53-R175H (via post-translational modifications), inducing an apoptotic program. Reference: Oncotarget. 2014 Oct 15;5(19):8879-92. https://pubmed.ncbi.nlm.nih.gov/25294809/

In vivo activity:

The safety and efficacy of NSC319726 were tested in a Galleria mellonella model of C. auris invasive candidiasis. Escalating single doses of NSC319726 up to 24 mg/kg were well tolerated by the uninfected larvae (100% survival until 7 days following injection). Doses of 6 and 12 mg/kg were selected for the G. mellonella model of C. auris infection. NSC319726 was effective in rescuing larvae infected with C. auris I.3 and IV.1 strains, with significantly improved survival rates, compared to the untreated group (Fig. 2). Reference: Microbiol Spectr. 2021 Dec 22;9(3):e0139521. https://pubmed.ncbi.nlm.nih.gov/34730380/

	Solvent	mg/mL	mM
Solubility
	DMF	16.0	68.28
	DMF:PBS (pH 7.2) (1:1)	0.5	2.13
	DMSO	21.9	93.55

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 234.32 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.

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. Sun N, Li D, Zhang Y, Killeen K, Groutas W, Calderone R. Repurposing an inhibitor of ribosomal biogenesis with broad anti-fungal activity. Sci Rep. 2017 Dec 5;7(1):17014. doi: 10.1038/s41598-017-17147-x. PMID: 29209049; PMCID: PMC5717060. 2. Yu X, Blanden AR, Narayanan S, Jayakumar L, Lubin D, Augeri D, Kimball SD, Loh SN, Carpizo DR. Small molecule restoration of wildtype structure and function of mutant p53 using a novel zinc-metallochaperone based mechanism. Oncotarget. 2014 Oct 15;5(19):8879-92. doi: 10.18632/oncotarget.2432. PMID: 25294809; PMCID: PMC4253404. 3. Li J, Coste AT, Bachmann D, Sanglard D, Lamoth F. Assessment of the In Vitro and In Vivo Antifungal Activity of NSC319726 against Candida auris. Microbiol Spectr. 2021 Dec 22;9(3):e0139521. doi: 10.1128/Spectrum.01395-21. Epub 2021 Nov 3. PMID: 34730380; PMCID: PMC8567239. 4. Yu X, Vazquez A, Levine AJ, Carpizo DR. Allele-specific p53 mutant reactivation. Cancer Cell. 2012 May 15;21(5):614-625. doi: 10.1016/j.ccr.2012.03.042. PMID: 22624712; PMCID: PMC3366694.

In vitro protocol:

In vivo protocol:

1. Li J, Coste AT, Bachmann D, Sanglard D, Lamoth F. Assessment of the In Vitro and In Vivo Antifungal Activity of NSC319726 against Candida auris. Microbiol Spectr. 2021 Dec 22;9(3):e0139521. doi: 10.1128/Spectrum.01395-21. Epub 2021 Nov 3. PMID: 34730380; PMCID: PMC8567239. 2. Yu X, Vazquez A, Levine AJ, Carpizo DR. Allele-specific p53 mutant reactivation. Cancer Cell. 2012 May 15;21(5):614-625. doi: 10.1016/j.ccr.2012.03.042. PMID: 22624712; PMCID: PMC3366694.

1: Yu, X., Vazquez, A., Levine, A.J., et al. Allele-specific p53 mutant reactivation. Cancer Cell 21(5), 614-625 (2012). 2: Sun, N., Li, D., Zhang, Y., et al. Repurposing an inhibitor of ribosomal biogenesis with broad anti-fungal activity. Sci. Rep. 7(1), 17014 (2017).