Identification | Back Directory | [Name]
DIM-C-pPhCO2Me | [CAS]
151358-48-4 | [Synonyms]
DIM-C-pPhCO2Me DIM-C-pPhCO2Me >=98% (HPLC) Benzoic acid, 4-(di-1H-indol-3-ylmethyl)-, methyl ester | [Molecular Formula]
C25H20N2O2 | [MDL Number]
MFCD31697720 | [MOL File]
151358-48-4.mol | [Molecular Weight]
380.44 |
Chemical Properties | Back Directory | [Melting point ]
98-100 °C | [Boiling point ]
618.6±50.0 °C(Predicted) | [density ]
1.287±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
DMSO:100.5(Max Conc. mg/mL);264.16(Max Conc. mM) Ethanol:38.0(Max Conc. mg/mL);99.88(Max Conc. mM) | [form ]
Solid | [pka]
16.34±0.30(Predicted) | [color ]
Light yellow to yellow |
Hazard Information | Back Directory | [Uses]
DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhCO2Me induces Apoptosis. DIM-C-pPhCO2Me decreases PAX3-FOXO1A, N-Myc, Rassf4, MyoD1, Grem1, and DAPK1 proteins. DIM-C-pPhCO2Me decreases expression of TXNDC5 and IDH1, induces markers of ER stress (CHOP, ATF4 and p-PERK). DIM-C-pPhCO2Me inhibits renal cell carcinoma, breast cancer. DIM-C-pPhCO2Me can also be used in rhabdomyosarcoma research[1][2][3][4][5]. | [Biological Activity]
DIM-C-pPhCO2Me is a NR4A1 (Nur77) antagonist th at exhibit potent anticancer activity in pancreaticcolonbreastkidneyand rhabdomyosarcoma cells. DIM-C-pPhCO2Me decreases expression of PAX3-FOXO1A and β1-integrin proteins in Rh30 rhabdomyosarcoma and MDA-MB-231 breast cancer cells. DIM-C-pPhCO2Me inhibits migration of Rh30 and MDA-MB-231 cancer cells.''DIM-C-pPhCO2Me is also known as 1,1-bis(3μ-indolyl)-1-(p-carboxymethylphenyl)methane. In pancreatic and colon cancer cellsDIM-C-pPhCO2Me plays an inhibitory role on cell migration. DIM-C-pPhCO2Me prevents the action of mechanistic target of rapamycin (mTOR) and reduces the multiplication and survival of cancer cells. It stimulates reactive oxygen species (ROS) in various cancer cell lines. | [in vivo]
DIM-C-pPhCO2Me (2 mg/kg, single dose, intratracheally, 30 min before E. coliinfection) results in augmented phagocytic activity of AMs and reduces the mortality of mice with E. coli pneumonia[5].
Animal Model: | Male mice with E. coli pneumonia[5] | Dosage: | 2 mg/kg, single dose | Administration: | intratracheally, 30 min before E. coli infection | Result: | Showed an obvious augmented phagocytic activity.
Reduced the mortality in mice undergoing E. coli pneumonia (36.6% vs. 75%).
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| [IC 50]
Nur77/NR4A1; IDH1 | [storage]
Store at -20°C | [References]
[1] Hedrick E, et al. Nuclear Receptor 4A1 (NR4A1) as a Drug Target for Renal Cell Adenocarcinoma. PLoS One. 2015 Jun 2;10(6):e0128308. DOI:10.1371/journal.pone.0128308 [2] Hedrick E, et al. Nuclear receptor 4A1 as a drug target for breast cancer chemotherapy. Endocr Relat Cancer. 2015 Oct;22(5):831-40. DOI:10.1530/ERC-15-0063 [3] Lacey A, et al. Interleukin-24 (IL24) Is Suppressed by PAX3-FOXO1 and Is a Novel Therapy for Rhabdomyosarcoma. Mol Cancer Ther. 2018 Dec;17(12):2756-2766. DOI:10.1158/1535-7163.MCT-18-0118 [4] Lacey A, et al. PAX3-FOXO1A Expression in Rhabdomyosarcoma Is Driven by the Targetable Nuclear Receptor NR4A1. Cancer Res. 2017 Feb 1;77(3):732-741. DOI:10.1158/0008-5472.CAN-16-1546 [5] Cui P, et al. Deficiency of the Transcription Factor NR4A1 Enhances Bacterial Clearance and Prevents Lung Injury During Escherichia Coli Pneumonia. Shock. 2019 Jun;51(6):787-794. DOI:10.1097/SHK.0000000000001184 |
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Company Name: |
Energy Chemical
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Tel: |
021-58432009 400-005-6266 |
Website: |
http://www.energy-chemical.com |
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