TC-E 5002Selective KDM2/7 inhibitor CAS# 1453071-47-0 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1453071-47-0 | SDF | Download SDF |
| PubChem ID | 71735843 | Appearance | Powder |
| Formula | C15H27NO4 | M.Wt | 285.38 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in 1eq. NaOH and to 100 mM in DMSO | ||
| Chemical Name | 3-[9-cyclopropylnonanoyl(hydroxy)amino]propanoic acid | ||
| SMILES | C1CC1CCCCCCCCC(=O)N(CCC(=O)O)O | ||
| Standard InChIKey | NEHSERYKENINRH-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C15H27NO4/c17-14(16(20)12-11-15(18)19)8-6-4-2-1-3-5-7-13-9-10-13/h13,20H,1-12H2,(H,18,19) | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | Selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). Inhibits growth of HeLa and KYSE-150 cancer cells in vitro. |
TC-E 5002 Dilution Calculator
TC-E 5002 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.5041 mL | 17.5205 mL | 35.041 mL | 70.082 mL | 87.6025 mL |
| 5 mM | 0.7008 mL | 3.5041 mL | 7.0082 mL | 14.0164 mL | 17.5205 mL |
| 10 mM | 0.3504 mL | 1.752 mL | 3.5041 mL | 7.0082 mL | 8.7602 mL |
| 50 mM | 0.0701 mL | 0.3504 mL | 0.7008 mL | 1.4016 mL | 1.752 mL |
| 100 mM | 0.035 mL | 0.1752 mL | 0.3504 mL | 0.7008 mL | 0.876 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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Histone demethylase KDM7A controls androgen receptor activity and tumor growth in prostate cancer.[Pubmed:30183076]
Int J Cancer. 2018 Dec 1;143(11):2849-2861.
Prostate cancer can be controlled by androgen-hormone treatment until the cancer becomes refractory. It is believed that hormone sensitivity is largely dependent on androgen receptor (AR) activity. Here, we found the histone demethylase KDM7A which demethylates histone H3K27 to be overexpressed in enzalutamide resistant castration-resistant prostate cancer cell line C4-2b, and investigated the molecular mechanism whereby androgen receptor activity is regulated by KDM7A. We engineered AR-positive LNCaP cells to stably express a short-hairpin RNA against KDM7A mRNA from a lentiviral vector. By measuring AR downstream gene expression after androgen stimulation, we found that a KDM7A-deficient cell line showed lower AR downstream gene expression compared to a control cell. KDM7A knock-down in LNCaP cell line caused decreased cell proliferation. Western blot analysis with modified-histone antibody revealed that the KDM7A-knock-down LNCaP cell line had increased H3K27 di-methylation. We confirmed KDM7A binding on AR target-gene promoters after hormone stimulation in chromatin-immunoprecipitation experiments. And increased H3K27 di-methylation was observed in KDM7A knock-down LNCaP stable cell. Treatment with KDM7A inhibitor, TC-E 5002, reduced proliferation and induced apoptosis of prostate cancer cells. Finally, we observed that the KDM7A protein was significantly upregulated in prostate cancer tissue, and that this difference correlated with the Gleason score. These data suggested that KDM7A is potentially a good therapeutic target for prostate cancer drugs and can be used as potentially a good prognostic indicator for prostate cancer and related treatment strategies.
Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.[Pubmed:23964788]
J Med Chem. 2013 Sep 26;56(18):7222-31.
Histone N(epsilon)-methyl lysine demethylases KDM2/7 have been identified as potential targets for cancer therapies. On the basis of the crystal structure of KDM7B, we designed and prepared a series of hydroxamate analogues bearing an alkyl chain. Enzyme assays revealed that compound 9 potently inhibits KDM2A, KDM7A, and KDM7B, with IC50s of 6.8, 0.2, and 1.2 muM, respectively. While inhibitors of KDM4s did not show any effect on cancer cells tested, the KDM2/7-subfamily inhibitor 9 exerted antiproliferative activity, indicating the potential for KDM2/7 inhibitors as anticancer agents.
