TCID Chemical Structure

TCID Chemical Structure
Molecular Weight: 283.92

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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 [1] UCH-L1 [1]
IC50 0.6 μM 75 μM
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Liu Y, et al. Chem Biol, 2003, 10(9), 837-846.

[2] Martínez-Villarreal J, et al. Glia, 2012, 60(9), 1356-1365

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02240875 Recruiting Ebola|Ebola Zaire University of Oxford|Wellcome Trust|National Institute of  ...more University of Oxford|Wellcome Trust|National Institute of Allergy and Infectious Diseases (NIAID) September 2014 Phase 1
NCT01466738 Completed Healthy Centocor Ortho Biotech Services, L.L.C. September 2011 Phase 1

Chemical Information

Download TCID SDF
Molecular Weight (MW) 283.92
Formula

C9H2Cl4O2

CAS No. 30675-13-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 23 mg/mL (81.0 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-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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