C-DIM12
- CAS No.
- 178946-89-9
- Chemical Name:
- C-DIM12
- Synonyms
- CS-2311;C-DIMI2;C-DIM12;C-DIM12, >98%;C-DIM12 (C-DIM-12;C-DIM12, 178946-89-9;C-DIM12 >=98% (HPLC);C-DIM12, 10 mM in DMSO;bis(3-indolyl)-4-chlorophenylmethane;3,3'-[(4-chlorophenyl)methylene]bis-1H-Indole
- CBNumber:
- CB03067198
- Molecular Formula:
- C23H17ClN2
- Molecular Weight:
- 356.85
- MDL Number:
- MFCD05625919
- MOL File:
- 178946-89-9.mol
| Melting point | 76-77 °C |
|---|---|
| Boiling point | 585.6±45.0 °C(Predicted) |
| Density | 1.324±0.06 g/cm3(Predicted) |
| storage temp. | 2-8°C(protect from light) |
| solubility | Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 35 mg/ml) |
| form | solid |
| pka | 16.40±0.30(Predicted) |
| color | Orange |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months. |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
C-DIM12 price More Price(18)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 22951 | C-DIM12 ≥98% | 178946-89-9 | 5mg | $50 | 2024-03-01 | Buy |
| Cayman Chemical | 22951 | C-DIM12 ≥98% | 178946-89-9 | 10mg | $94 | 2024-03-01 | Buy |
| Cayman Chemical | 22951 | C-DIM12 ≥98% | 178946-89-9 | 25mg | $209 | 2024-03-01 | Buy |
| Cayman Chemical | 22951 | C-DIM12 ≥98% | 178946-89-9 | 100mg | $583 | 2024-03-01 | Buy |
| Tocris | 5821 | C-DIM12 ≥98%(HPLC) | 178946-89-9 | 10 | $138 | 2021-12-16 | Buy |
C-DIM12 Chemical Properties,Uses,Production
Description
C-DIM12 is a para-phenyl-substituted diindolylmethane (C-DIM) that is an orally bioavailable activator of nuclear receptor-related protein 1 (Nurr1/NR4A2). It is selective for Nurr1, not activating Nur77, neuron-derived orphan receptor 1 (Nor1), or the retinoid X receptor (RXR) in parallel luciferase assays. C-DIM12 (2.5-10 μM) inhibits proliferation of Ku7 and 253J B-V bladder cancer cells in a dose-dependent manner and induces apoptosis of KU7 cells in a Nurr1-dependent manner. In an orthotopic nude mouse model, C-DIM12 suppresses bladder cancer cell growth by 44 and 59% at doses of 12.5 and 25 mg/kg, respectively. C-DIM12 has neuroprotective properties, preventing dopaminergic cell loss and reducing the expression of NF-κB in the substantia nigra pars compacta in an MPTP mouse model of Parkinson’s disease. It also has analgesic and anti-inflammatory activity in the tail immersion and carrageenan paw edema assays at a dose of 100 mg/kg, without causing ulcers in rats.
Uses
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].
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 |
| Animal Model: | MPTP-induced C57BL/6 male Parkinsonism mice [2] |
| Dosage: | 25 mg/kg/day, 14day |
| Administration: | Intragastric gavage (i.g.) |
| Result: | Protected against the loss of DA neurons in the substantia nigra pars compacta and DA terminals in the striatum, maintained a ramified phenotype in microglia, and suppressed activation of astrocytes. |
| Animal Model: | The ICR mice model of intracerebral hemorrhage induced by collagenase type VII[3] |
| Dosage: | 50 and 100mg/kg/day at a 24-h interval, three times |
| Administration: | Orally administration |
| Result: | Improved the recovery of neurological function and prevented neuron loss in the hematoma, while suppressed activation of microglia/macrophages and expression of inflammatory mediators interleukin-6 and CC chemokine ligand 2. Preserved axonal structures in the internal capsule and axonal transport function. Decreased of iNOS mRNA expression. |
| Animal Model: | MiaPaCa2 cells (Ctrl and NURR1-KO) orthotopic xenograft tumor models[1] |
| Dosage: | 30 mg/kg, 30 day |
| Administration: | Intraperitoneal injection (i.p.) |
| Result: | Inhibited tumor growth and ATG7 and ATG12 mRNA levels, and induced apoptosis. |
IC 50
Nurr1/NR4A2
storage
Store at -20°C
References
1) Inamoto et al. (2008), 1,1-Bis(3’-indolyl)-1-(p-chlorophenyl)methane activates the orphan nuclear receptor Nurr1 and inhibits bladder cancer growth; Mol Cancer Ther., 7 3825 2) Li et al. (2012), Structure-dependent activation of NR4A2 (Nurr1) by 1,1-bis(3’-indoyl)-1-(aromatic)methane analogs in pancreatic cancer cells; Biochem. Pharmacol., 83 1445 3) De Miranda et al. (2015), 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 kB; Mol. Pharmacol., 87 1021 4) De Miranda et al. (2013), Neuroprotective efficacy and pharmokinetic behavior of novel anti-inflammatory para phenyl substituted diindolylmethanes ina a mouse model of Parkinson’s disease; J. Pharmacol. Exp. Ther., 345 125
C-DIM12 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29808 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9911 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49734 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38630 | 58 | |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
