Antibodies
TCID
- 貨號 Cat. No.
- S7140
- 規格 Size
- 10mgã€200mg
- 品牌 Brand
- Selleckchem
Description
TCID
Catalog No.S7140
TCID is a DUB inhibitor for ubiquitin C-terminal hydrolase L3 with IC50 of 0.6 μM, 125-fold selective to L1.
| Size | Price | Stock | Quantity | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| |||||||||||
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | TCID is a DUB inhibitor for ubiquitin C-terminal hydrolase L3 with IC50 of 0.6 μM, 125-fold selective to L1. | |||||
|---|---|---|---|---|---|---|
| Targets | UCH-L3 | UCH-L1 | ||||
| IC50 | 0.6 μM | 75 μM [1] | ||||
| In vitro | TCID is selective for UCH-L3 over UCH-L1 by over 100-fold. [1] NU6027 (10 μM) does not promote YFP-GLT-1 accumulation in intracellular vesicles in transfected MDCK cells, while LDN-57444 (10 μM) promotes YFP-GLT-1 accumulation. NU6027 (10 μM) does not produce long-term lysosomal degradation of GLT-1, while LDN-57444 (10 μM) has such effect. [2] TCID (10 μM) diminishes GlyT2 ubiquitination in brainstem and spinal cord primary neurons, which is more pronounced when UCHL1 is inhibited and when cells are exposed to these inhibitors for longer periods. [3] | |||||
| In vivo | ||||||
| Features | TCID demonstrates selectivity for UCH-L3 over UCH-L1 by over 100-fold. | |||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Enzyme Inhibition Studies | Various concentrations (100 μM to 50 nM) of TCID dissolved in DMSO are each added to 2 mL of 1 nM UCH-L1 or 50 pM UCH-L3 in UCH reaction buffer and incubated at 25℃ for 30 min. Ubiquitin C-terminal hydrolysis activity is initiated by adding 2 μL of 50 μM ubiquitin-AMC. The reactions are monitored at 25℃ using a Hitachi F4500 fluorescence spectrophotometer. The AMC fluorophore is excited at 380 nm and the rates of release of free AMC are measured by monitoring the increase in fluorescence emission at 460 nm. The initial velocity Vo is measured for each reaction and plotted against TCID concentrations in order to determine the IC50 values using GraFit V.5 software. |
|---|
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01668537 | Recruiting | Smallpox | Bavarian Nordic | 2013-03 | Phase 2 |
| NCT01823640 | Completed | Common Cold | Radboud University | 2013-03 | Phase 1 |
| NCT01827371 | Recruiting | Smallpox | National Institute of Allergy and Infectious Diseases (NIAID) | 2013-06 | Phase 2 |
| NCT01866306 | Not yet recruiting | Asthma | Merck|U-BIOPRED Consortium | 2013-06 | Phase 1 |
| NCT01769573 | Recruiting | Healthy Volunteers | University of Wisconsin, Madison | 2013-07 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 283.92 |
|---|---|
| Formula | C9H2Cl4O2 |
| CAS No. | 30675-13-9 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | UCH-L3 Inhibitor |
| Solubility (25°C) * | In vitro | DMSO | 23 mg/mL (81 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 1H-Indene-1,3(2H)-dione, 4,5,6,7-tetrachloro- |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.28392 | 2.8392 | 5.6784 | 8.5176 |
