| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
NSC19630 targets the Werner syndrome helicase (WRN). WRN is a RecQ helicase involved in DNA repair and maintenance of genomic stability. By inhibiting WRN helicase activity (IC50 = 20 μM), NSC19630 disrupts DNA repair in cancer cells. It also reactivates mutant p53, restoring its tumor suppressor function and inducing apoptosis.
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| ln Vitro |
Saos-2-His273 cells with p53 mutation growth measured by MIRA-1 (25 μM; 48 hr) [1]. Mutant p53 and MIRA-1 (5 μM; 48 hours) both limit cell proliferation [1]. While MIRA-1 (10 μM; 48 hours) much less effectively inhibits p5 3 Saos-2 cells, it dramatically decreases the number of colonies in Saos-2 cells expressing his273 [1]. The fraction of Saos-2 and Saos-2-his273 cells with sub-g1 DNA content increases significantly when mutant p53 is present [1]. MIRA-1 (5 and 10 μM; 24 hours) Transduces SKOV-His175 Cells Cell Proliferation Assay
In vitro, NSC19630 is a selective inhibitor of WRN helicase with an IC50 of 20 μM. It shows selectivity over human RecQ helicases RECQ1 and BLM. It reactivates mutant p53 and induces apoptosis. It has antitumor effects. It induces apoptosis by inhibiting the mitochondrial membrane potential. |
| ln Vivo |
In vivo, NSC19630 has been shown to induce apoptosis and inhibit tumor growth in xenografts. It has been found to have no adverse effects on healthy cells. Its ability to reactivate mutant p53 and inhibit WRN helicase makes it a promising anticancer agent.
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| Enzyme Assay |
In vitro enzyme assays for NSC19630 measure its inhibition of WRN helicase activity. The compound is incubated with WRN helicase and a DNA substrate, and the unwinding of the DNA is monitored. Its selectivity for WRN over other helicases is assessed.
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| Cell Assay |
Cell Proliferation Assay
Cell Types: Saos-2-His273, H1299-His175, SKOV-His175 and SKOV-His273[1] Tested Concentrations: 25 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited cell expression of EGFP, MDM2 and Bax[1]. It grows in a mutant p53-dependent manner, with a survival rate of 18.5~39% without doxycycline and a survival rate of 71.5~87.5% with doxycycline. Apoptosis analysis Cell Types: Saos-2 and Saos-2-His273 cells [1] Tested Concentrations: 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: In the presence of the mutant, results in a substantial increase in the fraction of cells with sub-G1 DNA content Section 53 pages. In vitro cell-based assays for NSC19630 involve treating cancer cells with the compound and measuring its effects on cell viability and apoptosis. Its effects on p53 activity and WRN helicase function are assessed. Its effects on mitochondrial membrane potential are measured. |
| Animal Protocol |
In vivo animal experiments for NSC19630 have been conducted in tumor xenograft models. Tumor-bearing mice are treated with NSC19630, and tumor growth inhibition is monitored. Its apoptotic effects in tumor tissues are assessed.
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| ADME/Pharmacokinetics |
NSC19630 has a molecular weight of 183.16 and a molecular formula of C8H9NO4. It is a solid powder. Its purity is ≥98%. It is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
NSC19630 is for research use only and is not intended for human use. Its safety profile is being evaluated in preclinical studies. It has been found to have no adverse effects on healthy cells. Standard safety precautions should be taken when handling.
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| References | |
| Additional Infomation |
NSC19630 (MIRA-1) is a selective inhibitor of WRN helicase with an IC50 of 20 μM. It reactivates mutant p53 and induces apoptosis. It has antitumor effects and has been shown to inhibit tumor growth in xenografts. It has no adverse effects on healthy cells. It is a research compound for studying WRN helicase and p53 biology.
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| Molecular Formula |
C8H9NO4
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|---|---|
| Molecular Weight |
183.163
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| Exact Mass |
183.053
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| CAS # |
72835-26-8
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| PubChem CID |
227681
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| Appearance |
White to light yellow solid powder
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| Density |
1.307g/cm3
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| Boiling Point |
298.2ºC at 760 mmHg
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| Flash Point |
134.1ºC
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| Index of Refraction |
1.514
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| LogP |
-0.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
13
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| Complexity |
264
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YXEWPGYLMHXLPS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H9NO4/c1-2-8(12)13-5-9-6(10)3-4-7(9)11/h3-4H,2,5H2,1H3
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| Chemical Name |
(2,5-dioxopyrrol-1-yl)methyl propanoate
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| Synonyms |
NSC 19630; NSC-19630; NSC19630
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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 : ~100 mg/mL (~545.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (13.65 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 25.0 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: ≥ 2.5 mg/mL (13.65 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 25.0 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: ≥ 2.5 mg/mL (13.65 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 | 5.4597 mL | 27.2985 mL | 54.5971 mL | |
| 5 mM | 1.0919 mL | 5.4597 mL | 10.9194 mL | |
| 10 mM | 0.5460 mL | 2.7299 mL | 5.4597 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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