2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. TTT-28

TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) 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.

For research use only. We do not sell to patients.

TTT-28 Chemical Structure

TTT-28 Chemical Structure

CAS No. : 1609138-51-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 581 In-stock
Solution
10 mM * 1 mL in DMSO USD 581 In-stock
Solid
5 mg USD 460 In-stock
10 mg USD 750 In-stock
25 mg USD 1500 In-stock
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Based on 1 publication(s) in Google Scholar

TTT-28 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) 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[1].

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
1 μM
Compound: 28
Inhibition of human wild type P-gp expressed in BacMam virus infected human HeLa cells assessed as calcein-AM accumulation after 10 mins by flow cytometry
Inhibition of human wild type P-gp expressed in BacMam virus infected human HeLa cells assessed as calcein-AM accumulation after 10 mins by flow cytometry
[PMID: 24773054]
In Vitro

TTT-28 (0-100?μM; 72 hours) reverses ABCB1-mediated MDR in drug selected SW620/Ad300 cells and transfected HEK293/ABCB1 cells; the 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[1].
TTT-28 (10 μM; 2 hours) raises the ABCB1-mediated MDR and increased the accumulation of [3H]-paclitaxel in ABCB1 overexpressing cells[1].
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[1].
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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TTT-28 Related Antibodies

Cell Viability Assay[1]

Cell Line: SW620 cells, SW620/Ad300 cells
Concentration: 0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time: 72 hours
Result: Decreased the resistance fold of ABCB1 substrates (Paclitaxel, Doxorubicin, Vincristine) in SW620/Ad300 cells compared to SW620 cells.
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, it enhances the inhibitory effect of paclitaxel on the growth of SW620/Ad300 tumor and promoted apoptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5-10 week Male athymic NCR (nu/nu) nude mice ABCB1 overexpressing tumor xenograft model with SW620/Ad300 cells
Dosage: 30 mg/kg
Administration: Deliver orally; every 3rd day; 18 days
Result: Lead to higher intratumoral accumulation of paclitaxel in tumors.
Molecular Weight

573.66

Formula

C31H31N3O6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@@H](C(C)C)C1=NC(C(NC2=CC=CC=C2C(C3=CC=CC=C3)=O)=O)=CS1)C4=CC(OC)=C(OC)C(OC)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (435.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7432 mL 8.7160 mL 17.4319 mL
5 mM 0.3486 mL 1.7432 mL 3.4864 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7432 mL 8.7160 mL 17.4319 mL 43.5798 mL
5 mM 0.3486 mL 1.7432 mL 3.4864 mL 8.7160 mL
10 mM 0.1743 mL 0.8716 mL 1.7432 mL 4.3580 mL
15 mM 0.1162 mL 0.5811 mL 1.1621 mL 2.9053 mL
20 mM 0.0872 mL 0.4358 mL 0.8716 mL 2.1790 mL
25 mM 0.0697 mL 0.3486 mL 0.6973 mL 1.7432 mL
30 mM 0.0581 mL 0.2905 mL 0.5811 mL 1.4527 mL
40 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0895 mL
50 mM 0.0349 mL 0.1743 mL 0.3486 mL 0.8716 mL
60 mM 0.0291 mL 0.1453 mL 0.2905 mL 0.7263 mL
80 mM 0.0218 mL 0.1089 mL 0.2179 mL 0.5447 mL
100 mM 0.0174 mL 0.0872 mL 0.1743 mL 0.4358 mL
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TTT-28 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TTT-281609138-51-3TTT28TTT 28P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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