A939572
Based on 41 publication(s) in Google Scholar
A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.39%
- CAS 番号: 1032229-33-6
- 分子式: C20H22ClN3O3
- 分子量:387.86
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 A939572
More- Gastroenterology. 2024 Jan 24:S0016-5085(24)00064-7. [Abstract]
- Cancer Res. 2023 Jul 14;83(14):2387-2404. [Abstract]
- Nat Commun. 2025 Feb 1;16(1):1237. [Abstract]
- Nat Commun. 2024 Nov 21;15(1):10107. [Abstract]
- Nat Commun. 2024 Sep 27;15(1):8273. [Abstract]
- Acta Pharm Sin B. 2025 Feb;15(2):892-908. [Abstract]
- Cell Death Dis. 2025 Apr 14;16(1):291. [Abstract]
- Cancer Lett. 2025 Dec 21:639:218232. [Abstract]
- Int J Biol Sci. 2022 Oct 18;18(16):6114-6128. [Abstract]
- J Exp Med. 2020 Oct 5;217(10):e20200318. [Abstract]
- Sci China Life Sci. 2022 Feb;65(2):341-361. [Abstract]
- Oncogene. 2016 Jan 28;35(4):427-37. [Abstract]
- Mol Med. 2024 Feb 21;30(1):28. [Abstract]
- Br J Cancer. 2020 Jun;122(12):1837-1847. [Abstract]
- Cell Rep. 2020 Dec 1;33(9):108444. [Abstract]
- Cancer Cell Int. 2024 Oct 29;24(1):357. [Abstract]
- Cancer Cell Int. 2019 Apr 18:19:103. [Abstract]
- J Ethnopharmacol. 2026 Feb 28:357:120890. [Abstract]
- Biochem Pharmacol. 2025 Jun 26:240:117089. [Abstract]
- Mol Metab. 2021 Jun:48:101203. [Abstract]
- Cells. 2022 Nov 12;11(22):3580. [Abstract]
- Cancer Metab. 2025 Feb 7;13(1):6. [Abstract]
- Eur J Pharmacol. 2024 Jan 15:963:176249. [Abstract]
- Respir Res. 2023 Jan 10;24(1):8. [Abstract]
- Int J Mol Sci. 2023 Apr 6;24(7):6826. [Abstract]
- J Pathol. 2020 Dec;252(4):358-370. [Abstract]
- Biol Res. 2019 Dec 17;52(1):60. [Abstract]
- Front Pharmacol. 2018 Jan 4:8:960. [Abstract]
- Chem Biol Interact. 2026 May 27:112177. [Abstract]
- PLoS Pathog. 2018 Aug 17;14(8):e1007261. [Abstract]
- Stem Cells. 2018 Oct;36(10):1603-1616. [Abstract]
- Med Oncol. 2022 Dec 5;40(1):40. [Abstract]
- J Cell Mol Med. 2019 Mar;23(3):2064-2076. [Abstract]
- Funct Integr Genomics. 2023 Aug 23;23(3):280. [Abstract]
- Biochim Biophys Acta Mol Cell Biol Lipids. 2020 Feb;1865(2):158540. [Abstract]
- Front Oncol. 2021 Jul 27:11:698856. [Abstract]
- Hum Cell. 2024 Nov 4;38(1):13. [Abstract]
- Biol Pharm Bull. 2022 Apr 1;45(4):438-445. [Abstract]
- SSRN. 23 Nov 2020.
- bioRxiv. 2020 Mar.
- Oncotarget. 2018 Jan 24;9(15):12064-12078. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
生物活性
IC50: <4 nM (mSCD1), 37 nM (hSCD1)[1]
A939572 exhibits robust in vivo activity with dose-dependent desaturation index lowering effects[1]. A939572 is a small molecule that specifically inhibits SCD1 enzymatic activity. A939572 demonstrates a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5 (IC50s of 65 nM, 50 nM, 65 nM, and 6 nM, respectively). In A939572 (SCDi) treated Caki1 and A498 cells, all five ER stress related genes are expressed at significantly increased levels compared to DMSO+BSA control, and this elevated expression can be blocked with the addition of OA-BSA[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1032229-33-6
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性状 Solid
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分子量 387.86
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分子式 C20H22ClN3O3
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Color White to off-white
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SMILES
O=C(N1CCC(OC2=C(Cl)C=CC=C2)CC1)NC3=CC=CC(C(NC)=O)=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (41)
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Journal Impact Factor
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Most Recent
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Gastroenterology
2024 Jan 24:S0016-5085(24)00064-7. PMID: 38272100 -
Cancer Res
Retinol saturase mediates retinoid metabolism to impair a ferroptosis defense system in cancer cells. [Abstract]2023 Jul 14;83(14):2387-2404. PMID: 37184371 -
Nat Commun
PPARα-mediated lipid metabolism reprogramming supports anti-EGFR therapy resistance in head and neck squamous cell carcinoma. [Abstract]2025 Feb 1;16(1):1237. PMID: 39890801 -
Nat Commun
Acid-exposed and hypoxic cancer cells do not overlap but are interdependent for unsaturated fatty acid resources. [Abstract]2024 Nov 21;15(1):10107. PMID: 39572570 -
Nat Commun
Lipid droplets sequester palmitic acid to disrupt endothelial ciliation and exacerbate atherosclerosis in male mice. [Abstract]2024 Sep 27;15(1):8273. PMID: 39333556 -
Acta Pharm Sin B
Intestinal stearoyl-coenzyme A desaturase-inhibition improves obesity-associated metabolic disorders. [Abstract]2025 Feb;15(2):892-908. PMID: 40177566 -
Cell Death Dis
A targetable antioxidant defense mechanism to EZH2 inhibitors enhances tumor cell vulnerability to ferroptosis. [Abstract]2025 Apr 14;16(1):291. PMID: 40229247 -
Cancer Lett
YTHDF2-mediated stabilization of SREBF1 promotes lipid metabolic reprogramming and ferroptosis-associated radioresistance in anaplastic thyroid carcinoma. [Abstract]2025 Dec 21:639:218232. PMID: 41435981 -
Int J Biol Sci
Stearoyl-CoA Desaturase-1 dependent lipid droplets accumulation in cancer-associated fibroblasts facilitates the progression of lung cancer. [Abstract]2022 Oct 18;18(16):6114-6128. PMID: 36439884 -
J Exp Med
2020 Oct 5;217(10):e20200318. PMID: 32716519 -
Sci China Life Sci
2022 Feb;65(2):341-361. PMID: 34047913 -
Oncogene
Betulinic acid induces a novel cell death pathway that depends on cardiolipin modification. [Abstract]2016 Jan 28;35(4):427-37. PMID: 25893306
A939572 purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jan 28;35(4):427-37. [Abstract]
HeLa cells are treated with vehicle (DMSO) or 200 nM SCD-1 inhibitor for 40 h after which cells are analysed via TEM.
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Mol Med
G protein-coupled estrogen receptor activates PI3K/AKT/mTOR signaling to suppress ferroptosis via SREBP1/SCD1-mediated lipogenesis. [Abstract]2024 Feb 21;30(1):28. PMID: 38383297 -
Br J Cancer
Stearoyl-CoA-desaturase-1 regulates gastric cancer stem-like properties and promotes tumour metastasis via Hippo/YAP pathway. [Abstract]2020 Jun;122(12):1837-1847. PMID: 32350414 -
Cell Rep
Concurrent Mutations in STK11 and KEAP1 Promote Ferroptosis Protection and SCD1 Dependence in Lung Cancer. [Abstract]2020 Dec 1;33(9):108444. PMID: 33264619 -
Cancer Cell Int
Stearoyl CoA desaturase inhibition can effectively induce apoptosis in bladder cancer stem cells. [Abstract]2024 Oct 29;24(1):357. PMID: 39472909 -
Cancer Cell Int
SCD1 is required for EGFR-targeting cancer therapy of lung cancer via re-activation of EGFR/PI3K/AKT signals. [Abstract]2019 Apr 18:19:103. PMID: 31019378 -
J Ethnopharmacol
Paris polyphylla Smith var. yunnanensis-derived saponins potentiate the antitumor activity of GPX4 inhibitors. [Abstract]2026 Feb 28:357:120890. PMID: 41232632 -
Biochem Pharmacol
Ghrelin attenuates metabolic dysfunction-associated steatotic liver disease by activating glutamine metabolism via inhibition of the IRE1α-XBP-1 pathway. [Abstract]2025 Jun 26:240:117089. PMID: 40581331 -
Mol Metab
Loss of mitochondrial aconitase promotes colorectal cancer progression via SCD1-mediated lipid remodeling. [Abstract]2021 Jun:48:101203. PMID: 33676027 -
Cells
Targeting Wnt/β-Catenin Signaling Exacerbates Ferroptosis and Increases the Efficacy of Melanoma Immunotherapy via the Regulation of MITF. [Abstract]2022 Nov 12;11(22):3580. PMID: 36429010 -
Cancer Metab
CD36 inhibition enhances the anti-proliferative effects of PI3K inhibitors in PTEN-loss anti-HER2 resistant breast cancer cells. [Abstract]2025 Feb 7;13(1):6. PMID: 39920872 -
Eur J Pharmacol
Identification and experimental validation of Stearoyl-CoA desaturase is a new drug therapeutic target for osteosarcoma. [Abstract]2024 Jan 15:963:176249. PMID: 38070637 -
Respir Res
TGF-β1 promotes SCD1 expression via the PI3K-Akt-mTOR-SREBP1 signaling pathway in lung fibroblasts. [Abstract]2023 Jan 10;24(1):8. PMID: 36627645 -
Int J Mol Sci
Stearoyl-CoA Desaturases1 Accelerates Non-Small Cell Lung Cancer Metastasis by Promoting Aromatase Expression to Improve Estrogen Synthesis. [Abstract]2023 Apr 6;24(7):6826. PMID: 37047797 -
J Pathol
ZHX2 inhibits SREBP1c-mediated de novo lipogenesis in hepatocellular carcinoma via miR-24-3p. [Abstract]2020 Dec;252(4):358-370. PMID: 32770671 -
Biol Res
RASAL1 induces to downregulate the SCD1, leading to suppression of cell proliferation in colon cancer via LXRα/SREBP1c pathway. [Abstract]2019 Dec 17;52(1):60. PMID: 31847887 -
Front Pharmacol
SCD1 Confers Temozolomide Resistance to Human Glioma Cells via the Akt/GSK3β/β-Catenin Signaling Axis. [Abstract]2018 Jan 4:8:960. PMID: 29354058
A939572 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jan 4:8:960. [Abstract]
Western blot for p-Akt (Ser-473), Akt, p-GSK3β (Ser-9), GSK3β, β-catenin, and SCD1 in T98G-R cells treated with DMSO, A939572, MK2206, A939572 plus MK2206, LY294002 and A939572 plus LY294002.
A939572 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jan 4:8:960. [Abstract]
Western blot for p-Akt (Ser-473), Akt, p-GSK3β (Ser-9), GSK3β, β-catenin, and SCD1 in U87-R cells treated with DMSO, A939572, MK2206, A939572 plus MK2206, LY294002 and A939572 plus LY294002.
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Chem Biol Interact
Sulfur mustard exposure induces inflammatory injury by Dnmt3b-mediated DNA methylation via oleic acid accumulation in Treg cells. [Abstract]2026 May 27:112177. PMID: 42208724 -
PLoS Pathog
Stearoly-CoA desaturase 1 differentiates early and advanced dengue virus infections and determines virus particle infectivity. [Abstract]2018 Aug 17;14(8):e1007261. PMID: 30118512 -
Stem Cells
Runx1 Role in Epithelial and Cancer Cell Proliferation Implicates Lipid Metabolism and Scd1 and Soat1 Activity. [Abstract]2018 Oct;36(10):1603-1616. PMID: 29938858 -
Med Oncol
Upregulation of SCD1 by ErbB2 via LDHA promotes breast cancer cell migration and invasion. [Abstract]2022 Dec 5;40(1):40. PMID: 36471172 -
J Cell Mol Med
Inhibition of stearoyl CoA desaturase-1 activity suppresses tumour progression and improves prognosis in human bladder cancer. [Abstract]2019 Mar;23(3):2064-2076. PMID: 30592142
A939572 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Mar;23(3):2064-2076. [Abstract]
Cyclins D1, Rb, PCNA, Cdk4 and Cdk6 are down-regulated after either 24 h treatment of A939572 or siRNAs, while cyclin E1 is up-regulated.
A939572 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Mar;23(3):2064-2076. [Abstract]
Compared to the DMSO (0.25%) group, A939572 at concentrations of 6.4 and 12.8 μg/mL up-regulate E-cadherin expression and down-regulate N-cadherin expression.
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Funct Integr Genomics
Deltex E3 ubiquitin ligase 4 promotes thyroid cancer progression through stearoyl-CoA desaturase 1. [Abstract]2023 Aug 23;23(3):280. PMID: 37612343 -
Biochim Biophys Acta Mol Cell Biol Lipids
Trichothecin inhibits invasion and metastasis of colon carcinoma associating with SCD-1-mediated metabolite alteration. [Abstract]2020 Feb;1865(2):158540. PMID: 31678511 -
Front Oncol
A Novel Ferroptosis-Related Gene Model for Overall Survival Predictions of Bladder Urothelial Carcinoma Patients. [Abstract]2021 Jul 27:11:698856. PMID: 34386423 -
Hum Cell
Establishment and drug resistance characterization of paired organoids using human primary colorectal cancer and matched tumor deposit specimens. [Abstract]2024 Nov 4;38(1):13. PMID: 39495391 -
Biol Pharm Bull
Inhibition of Stearoyl-CoA Desaturase 1 Potentiates Anti-tumor Activity of Amodiaquine in Non-small Cell Lung Cancer. [Abstract]2022 Apr 1;45(4):438-445. PMID: 35110426 -
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Oncotarget
2018 Jan 24;9(15):12064-12078. PMID: 29552293
溶剤 & 溶解度
DMSO : 100 mg/mL (257.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
Cells are plated (0.5 or 1×105/well) in 24-well plates in triplicate. Cells are counted using a Coulter Particle Counter. Oleic acid-albumin is added to media at 5μMol. A939572 stocks are prepared in DMSO. Temsirolimus dosing is performed. Soft agar cultures are prepared by diluting 2× growth medium 1:1 in 1.5% Seaplaque®GTG® agarose, with 500 cells/plate in 60mm culture dishes. Colonies are stained with Giemsa and counted after 3wks[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
A498 cells are subcutaneously implanted in athymic nu/nu mice at 1×106 cells/mouse in 50% Matrigel. Tumors reach ~50 mm3 prior to 4 wk treatment. A939572 is re-suspended in strawberry flavored Kool-Aid® in sterilized H2O (0.2 g/mL) vehicle at 30 mg/kg in a 50 μL dose. Mice are orally fed by using a syringe to administer the 50 μL dose twice daily/mouse. This modified method is found to be effective and less stressful on the mice. Temsirolimus is solubilized in 30% ethanol/saline and administered via intraperitoneal injection at 10 mg/kg in a 50 μL dose once every 72 hrs/mouse. Tumor volumes are calculated using the formula 0.5236 (L*W*H) and body weight are measured every 3 days.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Xin Z, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302. [Content Brief]
[2]. von Roemeling CA, et al. Stearoyl-CoA desaturase 1 is a novel molecular therapeutic target for clear cell renal cell carcinoma. Clin Cancer Res. 2013 May 1;19(9):2368-80. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5782 mL | 12.8912 mL | 25.7825 mL | 64.4562 mL |
| 5 mM | 0.5156 mL | 2.5782 mL | 5.1565 mL | 12.8912 mL | |
| 10 mM | 0.2578 mL | 1.2891 mL | 2.5782 mL | 6.4456 mL | |
| 15 mM | 0.1719 mL | 0.8594 mL | 1.7188 mL | 4.2971 mL | |
| 20 mM | 0.1289 mL | 0.6446 mL | 1.2891 mL | 3.2228 mL | |
| 25 mM | 0.1031 mL | 0.5156 mL | 1.0313 mL | 2.5782 mL | |
| 30 mM | 0.0859 mL | 0.4297 mL | 0.8594 mL | 2.1485 mL | |
| 40 mM | 0.0645 mL | 0.3223 mL | 0.6446 mL | 1.6114 mL | |
| 50 mM | 0.0516 mL | 0.2578 mL | 0.5156 mL | 1.2891 mL | |
| 60 mM | 0.0430 mL | 0.2149 mL | 0.4297 mL | 1.0743 mL | |
| 80 mM | 0.0322 mL | 0.1611 mL | 0.3223 mL | 0.8057 mL | |
| 100 mM | 0.0258 mL | 0.1289 mL | 0.2578 mL | 0.6446 mL |
A939572 関連分類
HY-50709 関連分類
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