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TTT-28

Catalog No. T13222   CAS 1609138-51-3

TTT-28 is a thiazole-valine peptidomimetic, and is a selective ABCB1 (P-gp/MDR1) inhibitor with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.

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TTT-28 Chemical Structure
TTT-28, CAS 1609138-51-3
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TTT-28 is a thiazole-valine peptidomimetic, and is a selective ABCB1 (P-gp/MDR1) inhibitor with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.
In vitro In drug selected SW620/Ad300 cells, TTT-28 (0-100?μM; 72 hours) reverses ABCB1-mediated MDR and transfected HEK293/ABCB1 cells(IC50s of TTT-28 in CCD-18Co, SW620 and SW620/Ad300 cells are 213.4±11.0 μM, 89.4±3.9 μM and 92.0±5.0?μM, respectively). TTT-28 (10 μM; 2 hours) raises the ABCB1-mediated MDR and increased the accumulation of [3H]-paclitaxel in ABCB1 overexpressing cells. TTT-28 (10 μM; 0-72 hours) does not interfer with the expression level and localization of ABCB1, it results from blocking the efflux function of ABCB1. TTT-28 (0-40?μM; 2 hours) interacts at the drug-substrate-binding site and actives the ATPase activity of ABCB1 in a concentration-dependent fashion.
In vivo TTT-28 (deliver orally; 30 mg/kg; every 3 rd day; 18 days) potentiates the anticancer activity of paclitaxel due to its inhibitory effect on the efflux function of ABCB1, TTT-28 enhances the inhibitory effect of paclitaxel on the growth of SW620/Ad300 tumor and promoted apoptosis.
Molecular Weight 573.66
Formula C31H31N3O6S
CAS No. 1609138-51-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Wang YJ, et al. Thiazole-valine peptidomimetic (TTT-28) antagonizes multidrug resistance in vitro and in vivo by selectively inhibiting the efflux activity of ABCBSci Rep. 2017 Feb 9;7:42106.

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Keywords

TTT-28 1609138-51-3 Others TTT 28 TTT28 inhibitor inhibit

 

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