MCB-613

SKU: orb1223415

Description

MCB-613 is a potent Steroid Receptor Coactivator Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death. MCB-613 can super-stimulate SRCs' transcriptional activity. MCB-613 increases SRCs' interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 selectively induce excessive stress in cancer cells. Over-stimulating the SRC oncogenic program can be an effective strategy to kill cancer cells. By integrating growth pathways on which cancer cells rely, steroid receptor coactivators (SRC-1, SRC-2, and SRC-3) represent emerging targets in cancer therapeutics.

Key Properties

• CAS Number: 1162656-22-5
• MW: 304.39
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₀N₂O
• SMILES: C1(C/C(=C\c2cnccc2)/C(=O)/C(=C/c2cnccc2)/C1)CC
• Target: Hydroxylase
• Solubility: DMSO : 50 mg/mL 164.26 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  MCB-613 (intravenous injection; 20 mg/kg; 3 times/week; 7 weeks) significantly and dramatically stalls the growth of the tumor compared with the control group and causes no obvious animal toxicity. Animal model: MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads). Dosage: 20 mg/kg. Administration: Intravenous injection; 20 mg/kg; 3 times/week; 7 weeks. Result: Inhibited tumor growth In vivo.
• In Vitro:
  MCB-613 (6-8 μM; 24 hours) activates endogenous MMP13 mRNA expression in MDA-MB-231 cells. MCB-613 (2-10 μM; 4 hours) leads to proteasome dysfunction and ER stress, the induction of the markers for unfolded protein response (UPR), including the phosphorylation of eIF2α and IRE1α as well as the induction of ATF4 protein expression. MCB-613 (0-7 μM; 4 hours) affects SRC-3 KO and WT HeLa cell viability, SRC-3 WT HeLa cell is more affected by MCB-613 compared with KO cells. RT-PCR Cell line: MDA-MB-231 cells. Concentration: 6 μM; 8 μM. Incubation time: 24 hours. Result: Increased MMP13 mRNA expression. Western blot analysis. Cell line: HeLa cells. Concentration: 2 μM; 4 μM; 6 μM; 8 μM; 10 μM. Incubation time: 24 hours. Result: Induced the p-eIF2α, p-IRE1α, and ATF-4 protein expression. Cell Viability Assay Cell line: SRC-3 KO and WT HeLa cells. Concentration: 3 μM; 4 μM; 5 μM; 6 μM; 7 μM. Incubation time: 24 hours. Result: Decreased SRC-3 KO and WT HeLa cell viability.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MCB-613 | MCB 613 | MCB613

Quick Database Links

Gene Symbol

Hydroxylase