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MedChemExpress - Model C-DIM12 - ...

MedChemExpress - Model C-DIM12 - 178946-89-9

C-DIM12 is a potent, orally active Nurr1 antagonist. C-DIM12 inhibits the tumor growth and autophagy, and induces the cell apoptosis. C-DIM12 has anti-inflammatory and neuroprotective effects, and can be used for cancer and neurological disease study[1][2][3].

C-DIM12

MCE China：C-DIM12

Brand：MedChemExpress (MCE)

Cat. No.HY-19808

CAS：178946-89-9

Synonyms：DIM-C-pPhCl

Purity：98.32%

Storage：4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：C-DIM12 is a potent, orally active Nurr1 antagonist. C-DIM12 inhibits the tumor growth and autophagy, and induces the cell apoptosis. C-DIM12 has anti-inflammatory and neuroprotective effects, and can be used for cancer and neurological disease study.

In Vitro：C-DIM12 (15 μM, 3-5 day) increases cell proliferation and survival by inhibiting autophagy in MiaPaCa2 cells[1].

In Vivo：C-DIM12 (25 mg/kg for i.p., 14 day) modulates glial reactivity in MPTP-Induced Parkinsonism mice[2]. C-DIM12 (50-100 mg/kg for i.p., three times ) attenuates brain inflammation and improves functional recovery after intracerebral hemorrhage in mice[3]. C-DIM12 (30 mg/kg for i.p., 30 day) inhibits tumor growth and autophagy, and induces apoptosis in NURR1-KO cells orthotopic xenograft[1]. Pharmacokinetic Analysis in C57BL/6 male mice[1] Route Organ Dose (mg/kg) Area under Curve (ng/mL*min) t1/2 (min) Cmax (ng/mL) i.g. Plasma 25 539,220 249 1120 i.g. Brain 25 2,273,711 265 3622

IC50 & Target：Nurr1/NR4A2

References：

[1]. Zarei M, et al. Nuclear Receptor 4A2 (NR4A2/NURR1) Regulates Autophagy and Chemoresistance in Pancreatic Ductal Adenocarcinoma. Cancer Res Commun. 2021;1(2):65-78. [Content Brief]

[2]. Sean L. Hammond, et al. The Nurr1 Ligand,1,1-bis(3′-Indolyl)-1-(p-Chlorophenyl)Methane, Modulates Glial Reactivity and Is Neuroprotective in MPTP-Induced Parkinsonism. J Pharmacol Exp Ther. 2018 Jun; 365(3): 636–651.

[3]. Keita Kinoshita, et al. A Nurr1 ligand C-DIM12 attenuates brain inflammation and improves functional recovery after intracerebral hemorrhage in mice. Sci Rep. 2022; 12: 11009.

[4]. De Miranda BR, et al. The Nurr1 Activator 1,1-Bis(3'-Indolyl)-1-(p-Chlorophenyl)Methane Blocks Inflammatory Gene Expression in BV-2 Microglial Cells by Inhibiting Nuclear Factor κB. Mol Pharmacol. 2015 Jun;87(6):1021-34. doi: 10.1124/mol.114.095398. Epub 2015 Apr 9. [Content Brief]

[5]. Hammond SL, et al. A novel synthetic activator of Nurr1 induces dopaminergic gene expression and protects against 6-hydroxydopamine neurotoxicity in vitro. Neurosci Lett. 2015 Oct 21;607:83-9. [Content Brief]

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