MeTC7 |
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Catalog No.GC52325
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MeTC7 is a vitamin D receptor (VDR) antagonist (IC50=2.9μM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1817841-22-7
Sample solution is provided at 25 µL, 10mM.
MeTC7 is a vitamin D receptor (VDR) antagonist (IC50=2.9μM). MeTC7 blocks VDR/RXRα, VDR/MYCN and VDR/PD-L1 signaling. MeTC7 inhibits tumor cell viability, colony formation and PD-L1 expression. MeTC7 can be used in research on neuroblastoma, ovarian cancer, acute myeloid leukemia and other tumors, as well as tumor immunotherapy[1-4].
In vitro, treatment with 100-500nM MeTC7 for 48 hours reduced PD-L1 protein level, reduced cell viability, and reduced colony number and size in AML-1, MV-411 and THP-1 cells[5]. Treatment with 100-500nM MeTC7 for 48 hours reduced PD-L1 surface expression and reduced cell viability in PANC-1 cells, KCKO cells and ES2 cells[6]. Pretreatment with 10μM MeTC7 for 30 minutes followed by electric pulse stimulation for 24 hours increased IL-6 mRNA expression, increased p-STAT3/STAT3 ratio, and increased myostatin and C/EBPδ mRNA expression in C2C12 cells[7].
In vivo, intraperitoneal injection of 10mg/kg MeTC7 for 7 days slowed tumor growth in NSG mice subcutaneously inoculated with ES2, SKOV-3 or D283 cells[8]. Intraperitoneal injection of 10mg/kg MeTC7 three times weekly for 4 weeks increased the proportion of spleen Th17 cells and CD4+RORyt+ cells, elevated serum IL-17A and IL-22 levels, upregulated prostate RORyt mRNA expression, promoted prostate inflammatory cell infiltration, and reduced prostate VDR and p-ERK1/2 expression in NOD mouse experimental autoimmune prostatitis model[9].
References:
[1] Liang L, Ruan Y, Yu X, et al. DKS26 Alleviates Ischemia-Reperfusion Injury-Induced Acute Kidney Injury by Stabilizing Vitamin D Receptors to Inhibit the Inflammatory Pathway of NF-κB P65. Int J Mol Sci. 2025 Mar 25;26(7):2985.
[2] Lee TW, Lee TI, Higa S, et al. Calcitriol deficiency reduces myocardial ATP production with disturbed mitochondrial dynamics and increased uncoupling protein 2 expression. Eur J Pharmacol. 2025 Sep 5;1002:177858.
[3] Dong L, Gao Y, Li Q, et al. Betulinic Acid Enema Alleviates Colitis by Targeting Vitamin D Receptor to Protect the Intestinal Mucosal Barrier and Modulate Mucosa-Associated Microbiota. Phytother Res. 2026 Jun 18.
[4] Isaac I, Patel L, Tran N,et al. Reengineering Endogenous Targeting Lipid Nanoparticles (ENDO) for Systemic Delivery of mRNA to Pancreas. Adv Mater. 2025 Oct;37(40):e2507657.
[5] Khazan N, Quarato ER, Singh NA, et al. Vitamin D Receptor Antagonist MeTC7 Inhibits PD-L1. Cancers. 2023 Jun 30;15(13):3432.
[6] Singh RK, Kim K, Rowswell-Turner RB, et al. Targeting Vitamin-D receptor(VDR) by a small molecule antagonist MeTC7 inhibits PD-L1 but controls TH-MYCN neuroblastoma growth PD-L1 independently. bioRxiv. 2020 Aug 17:2020.08.16.252940.
[7] Hashimoto S, Hosoi T, Yakabe M, et al. Exercise-induced vitamin D receptor and androgen receptor mediate inhibition of IL-6 and STAT3 in muscle. Biochem Biophys Rep. 2024;37:101621.
[8] Khazan N, Kim KK, Hansen JN, et al. Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors In Vivo. J Med Chem. 2022 Apr 28;65(8):6039-55.
[9] Niu D, Yue SY, Wang X, et al. A high-glucose diet aggravates experimental autoimmune prostatitis via DHVD3/VDR/ERK axis-mediated Th17 differentiation. Asian J Androl. 2026;28:1-11.
| Cell experiment [1]: | |
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Cell lines |
C2C12 myotubes (murine myoblast cell line) |
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Preparation Method |
C2C12 cells were differentiated into myotubes in DMEM with 2% horse serum for 5 days. Differentiated C2C12 myotubes were pretreated with 10μM MeTC7 for 30 minutes before electric pulse stimulation (EPS) at 1Hz, 2ms, 11.5V for 24 hours. After EPS, cells were collected for mRNA expression analysis of IL-6, myostatin, and C/EBPδ by qRT-PCR, and for p-STAT3 and total STAT3 protein level measurement by Western blot. |
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Reaction Conditions |
10μM; 30min pretreatment + 24h EPS |
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Applications |
MeTC7 increased IL-6 mRNA expression compared with EPS alone. MeTC7 increased p-STAT3/STAT3 ratio. MeTC7 increased myostatin and C/EBPδ mRNA expression. |
| Animal experiment [2]: | |
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Animal models |
Male non-obese diabetic (NOD) mice with experimental autoimmune prostatitis (EAP) fed 20% glucose water |
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Preparation Method |
Mice were intraperitoneally administered MeTC7 10mg/kg three times weekly for 4 weeks after the first immunization. Prostate tissue, spleen lymphocytes, and serum were collected at sacrifice for histological scoring, flow cytometry, ELISA, RT-qPCR and immunohistochemistry. |
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Dosage form |
10mg/kg; i.p.; three times weekly for 4 weeks |
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Applications |
MeTC7 increased the proportion of spleen Th17 cells and CD4+RORyt+ cells. MeTC7 elevated serum IL-17A and IL-22 levels. MeTC7 upregulated prostate RORyt mRNA expression. MeTC7 promoted prostate inflammatory cell infiltration. MeTC7 reduced prostate VDR and p-ERK1/2 expression. |
References: [1] Hashimoto S, Hosoi T, Yakabe M, et al. Exercise-induced vitamin D receptor and androgen receptor mediate inhibition of IL-6 and STAT3 in muscle. Biochem Biophys Rep. 2024 Mar;37:101621. [2] Niu D, Yue SY, Wang X, et al. A high-glucose diet aggravates experimental autoimmune prostatitis via DHVD3/VDR/ERK axis-mediated Th17 differentiation. Asian J Androl. 2026;28:1-11. | |
| Cas No. | 1817841-22-7 | SDF | |
| Canonical SMILES | C[C@@]12[C@](C=C[C@@]34C2CC[C@@]5(C)[C@@]3([H])CC[C@]5([H])[C@@H](CCCC(C)C)C)(N6C(N(C)C(N64)=O)=O)C[C@@H](OC(CBr)=O)CC1 | ||
| Formula | C32H48BrN3O4 | M.Wt | 618.7 |
| Solubility | Ethanol: 1 mg/ml | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6163 mL | 8.0815 mL | 16.1629 mL |
| 5 mM | 323.3 μL | 1.6163 mL | 3.2326 mL |
| 10 mM | 161.6 μL | 808.1 μL | 1.6163 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)