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NCATS-SM0225
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Catalog No. T217875 Copy Product Info
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NCATS-SM0225 is an ER-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, VDAC2, and VDAC3. It has an IC50 of 1.02 μM for ERAD inhibition and a Kd of 3.13 μM for binding to human VDAC1. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling, and activates PERK. The compound selectively kills cancer cells and has shown tumor growth inhibition in melanoma xenograft models. It is useful for research into various cancers, including melanoma, as well as studies on ERAD and calcium homeostasis regulatory mechanisms.
NCATS-SM0225
Cas No. 1212623-02-3
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | NCATS-SM0225 is an ER-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, VDAC2, and VDAC3. It has an IC50 of 1.02 μM for ERAD inhibition and a Kd of 3.13 μM for binding to human VDAC1. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling, and activates PERK. The compound selectively kills cancer cells and has shown tumor growth inhibition in melanoma xenograft models. It is useful for research into various cancers, including melanoma, as well as studies on ERAD and calcium homeostasis regulatory mechanisms. |
| Targets & IC50 | VDAC1:3.13 μM (Kd) |
| In vitro | NCATS-SM0225 directly binds to recombinant human VDAC1 and shows a Kd of 3.13 μM, as determined by MST [1]. In HeLa cells, NCATS-SM0225 (2 μM; 1 h) associates with VDAC1, VDAC2, and VDAC3, which is evidenced by increased thermodynamic stability of these proteins. At concentrations of 100-400 nM, NCATS-SM0225 modulates VDAC1 channel activity by promoting voltage-dependent closure at lower negative potentials, with a functional IC50 of 140 nM. Additionally, NCATS-SM0225 (0.625-5 μM; 6 h) robustly inhibits ER misfolding in HeLa cells, indicated by an IC50 of 1.02 μM in NHK-drGFP reporter assays. The compound (0.625-5 μM; 6-22 h) raises calcium levels in the mitochondria, cytosol, and endoplasmic reticulum of HeLa cells in a VDAC-dependent manner, with greater effects seen at higher concentrations and longer incubation times. Within 40-48 hours, NCATS-SM0225 (0-10 μM) selectively induces apoptotic cell death in certain cancer cell lines without harming normal cells; this selectivity is linked to disrupting calcium homeostasis and degrading ERAD complex proteins. In HeLa cells, NCATS-SM0225 (1.25-10 μM; 6-24 h) dose- and time-dependently, and calcium 2+ dependently, degrades ERAD complex proteins (HERP1, OS9, FAM8A1) while activating the PERK signaling pathway. |
| In vivo | NCATS-SM0225 (20 mg/kg; administered intraperitoneally; once daily for 14 days) significantly inhibits the growth of A375 melanoma xenografts in male BALB/c-nu mice without any detectable toxicity. |
| Molecular Weight | 460.61 |
| Formula | C23H28N2O4S2 |
| Cas No. | 1212623-02-3 |
| Smiles | C[C@]12[C@@]([C@@]3([C@@](CC1)([C@H](C)C(=O)O3)[H])[H])([C@H](C)C4=C(C2)SC(NS(CC5=CC=CC=C5)(=O)=O)=N4)[H] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Related Tags: NCATS-SM0225 in vivo | NCATS-SM0225 in vitro | NCATS-SM0225 formula | NCATS-SM0225 molecular weight
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