TCH-165 is a small molecule modulator of proteasome assembly , which increases 20S levels and facilitates 20S -mediated protein degradationIn VitroTCH-165 (0.01-10 μM; 72 hours; RPMI8226 and U87MG cells) treatment inhibits cell growth of RPMI8226 and U87MG cells with IC 50 of 1.6 μM and 2.4 μM, respectively. ?/nTCH-165 (0-10 μM; 24 hours; HEK293T cells) treatment enhances ODC degradation is blocked by BTZ indicated that this event is proteasome-mediated. TCH-165 enhances proteolytic degradation in a concentration-dependent manner. ?/nTCH-165 enhances the chymotrypsin-like (CT-L), trypsin-like (Tryp-L) and caspase-like (Casp-L) activities with EC 50 s of 4.2 μM, 3.2 μM and 4.7 μM, respectively. ?/nTCH-165 enhances 20S-mediated degradation of IDPs, α-syn, and tau in vitro, and does not induce the degradation of structured proteins such as GAPDH. ?/nTCH-165-treated cells display a decrease in the assembled 26S and an increase in the 20S proteasome. TCH-165 regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: RPMI8226 and U87MG cells Concentration: 0.01-10 μM Incubation Time: 72 hours Result: Inhibited cell growth of RPMI8226 and U87MG cells with IC 50 of 1.6 μM and 2.4 μM, respectively. Western Blot AnalysisCell Line: HEK293T cells Concentration: 0 μM, 3 μM, 10 μM Incubation Time: 24 hours Result: Enhanced proteolytic degradation in a concentration-dependent manner.Form:SolidIC50& Target:Proteasome assembly. Specification: 0.99 Molecular Formula: C39H37N3O3 Molecular Weight: 595.7 PubChem CID: 71762768 Isomeric 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
- UPC:
- 12352200
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- T650057-50mg
- CAS:
- 1446350-60-2
- Product Size:
- 50mg
