CBB1003

CAS# 1379573-88-2

CBB1003

Catalog No. BCC5524----Order now to get a substantial discount!

Product Name & Size Price Stock
CBB1003: 5mg $368 In Stock
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Chemical structure

CBB1003

3D structure

Chemical Properties of CBB1003

Cas No. 1379573-88-2 SDF Download SDF
PubChem ID 57345268 Appearance Powder
Formula C25H31N9O4 M.Wt 521.57
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
Chemical Name 4-[[3-[4-(4-carbamimidoylbenzoyl)piperazine-1-carbonyl]-5-nitrophenyl]methyl]piperazine-1-carboximidamide
SMILES C1CN(CCN1CC2=CC(=CC(=C2)C(=O)N3CCN(CC3)C(=O)C4=CC=C(C=C4)C(=N)N)[N+](=O)[O-])C(=N)N
Standard InChIKey SKTVJNLOILHEKO-UHFFFAOYSA-N
Standard InChI InChI=1S/C25H31N9O4/c26-22(27)18-1-3-19(4-2-18)23(35)31-9-11-32(12-10-31)24(36)20-13-17(14-21(15-20)34(37)38)16-30-5-7-33(8-6-30)25(28)29/h1-4,13-15H,5-12,16H2,(H3,26,27)(H3,28,29)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

CBB1003 Dilution Calculator

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CBB1003 Molarity Calculator

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Preparing Stock Solutions of CBB1003

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9173 mL 9.5864 mL 19.1729 mL 38.3458 mL 47.9322 mL
5 mM 0.3835 mL 1.9173 mL 3.8346 mL 7.6692 mL 9.5864 mL
10 mM 0.1917 mL 0.9586 mL 1.9173 mL 3.8346 mL 4.7932 mL
50 mM 0.0383 mL 0.1917 mL 0.3835 mL 0.7669 mL 0.9586 mL
100 mM 0.0192 mL 0.0959 mL 0.1917 mL 0.3835 mL 0.4793 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on CBB1003

CBB1003, a lysine-specific demethylase 1 inhibitor, suppresses colorectal cancer cells growth through down-regulation of leucine-rich repeat-containing G-protein-coupled receptor 5 expression.[Pubmed:25060070]

J Cancer Res Clin Oncol. 2015 Jan;141(1):11-21.

PURPOSE: Lysine-specific demethylase 1 (LSD1) was highly expressed in several malignancies and had been implicated in pathological processes of cancer cells. However, the role of LSD1 in colorectal cancer (CRC) carcinogenesis, prognosis and treatment remains uncharacterized. METHODS: In this study, we examined LSD1 expression in paraffin-embedded CRC specimens from 295 patients, including 65 patients with paired samples of colorectal carcinoma, adjacent adenoma and normal colorectal tissues. Using an LSD1 inhibitor, CBB1003, as a probe, we studied the association between LSD1 and leucine-rich repeat-containing G-protein-coupled receptor 5 (LGR5), a CRC stem cell marker involved in carcinogenesis. The anti-tumor effects of CBB1003 on CRC cells were also examined. RESULTS: LSD1 expression was significantly elevated in colorectal tumor tissues compared with adjacent adenoma and normal colorectal tissues (P < 0.001), and LSD1 levels were significantly correlated with an advanced AJCC T stage (P = 0.012) and distant metastasis (P = 0.004). CBB1003 inhibited CRC cell proliferation and colony formation. In cultured CRC cells, inhibiting LSD1 activity by CBB1003 caused a decrease in LGR5 levels while overexpression of LGR5 reduced CBB1003-induced cell death. We also observed the inactivation of beta-catenin/TCF signaling after CBB1003 treatment, consistent with the positive correlations among LSD1, LGR5, beta-catenin and c-Myc expression in human colon tumor and adenoma tissues. CONCLUSION: Our result suggested that LSD1 overexpression promotes CRC development and that the LSD1 inhibitor inhibits CRC cell growth by down-regulating LGR5 levels and inactivates the Wnt/beta-catenin pathway. Thus, LSD1 and its inhibitor might provide a new target or a useful strategy for therapy of CRC.

Description

CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.

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