| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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Purity: ≥98%
TCH-165 (TCH165) is a novel and potent small molecule modulator of proteasome assembly, which can lead to an increase in 20S levels. The increase in the level of free 20S corresponds to enhanced proteolysis of IDPs.
| ln Vitro |
TCH-165 (0.01-10 μM; 72 hours) inhibits RPMI8226 and U87MG cell growth, with IC50 values of 1.6 μM and 2.4 μM, in that order [1]. TCH-165 (0–10 μM; 24 hours; HEK293T cells) Boosts ODC TCH-165, in a concentration-dependent way, boosts proteolysis [1]. TCH-165 improves the affinity of chymotrypsin-like (CT-L), trypsin-like (Tryp-L), and caspase-like (Casp). It also improves α-syn, tau, and 20S-mediated IDPs. However, it does not improve the affinity of structural proteins like GAPDH [1]. -L) activity, the corresponding EC50 values are 4.2 μM, 3.2 μM, and 4.7 μM [1]. Cells treated with TCH-165 displayed an increase in 20S proteasome and a decrease in reconstituted 26S proteasome. TCH-165 promotes 20S-mediated protein degradation by controlling the dynamic equilibrium between 26S and 20S proteasome complexes [1]. [1]
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: RPMI8226 and U87MG cells Tested Concentrations: 0.01-10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibits the growth of RPMI8226 and U87MG cells with IC50 of 1.6 μM and 2.4 μM respectively. Western Blot Analysis[1] Cell Types: HEK293T Cell Tested Concentrations: 0 μM, 3 μM, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Proteolytic degradation is enhanced in a concentration-dependent manner. |
| References |
| Molecular Formula |
C39H37N3O3
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|---|---|
| Molecular Weight |
595.7294
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| Exact Mass |
595.28
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| Elemental Analysis |
C, 78.63; H, 6.26; N, 7.05; O, 8.06
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| CAS # |
1446350-60-2
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| PubChem CID |
71762768
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
7.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
45
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| Complexity |
937
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCOC(=O)[C@]1([C@H](N(C(=N1)C2=CC=C(C=C2)OC)CC3=CC=CC=C3)C4=CC=C(C=C4)NCC5=CC=CC=C5)C6=CC=CC=C6
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| InChi Key |
XXDLWRCUPASJGY-VQIIKMDRSA-N
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| InChi Code |
InChI=1S/C39H37N3O3/c1-3-45-38(43)39(33-17-11-6-12-18-33)36(31-19-23-34(24-20-31)40-27-29-13-7-4-8-14-29)42(28-30-15-9-5-10-16-30)37(41-39)32-21-25-35(44-2)26-22-32/h4-26,36,40H,3,27-28H2,1-2H3/t36-,39-/m0/s1
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| Chemical Name |
Ethyl (4S,5S)-1-benzyl-5-(4-(benzylamino)phenyl)-2-(4-methoxyphenyl)-4-phenyl-4,5-dihydro-1H-imidazole-4-carboxylate
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| Synonyms |
TCH-165 TCH 165 TCH165
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~419.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (10.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (10.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6786 mL | 8.3931 mL | 16.7861 mL | |
| 5 mM | 0.3357 mL | 1.6786 mL | 3.3572 mL | |
| 10 mM | 0.1679 mL | 0.8393 mL | 1.6786 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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