HhAntag

SKU: orb1223112

Description

HhAntag is a GLI1-mediated transcription inhibitor. It acts as an inhibitor of the Shh pathway.

Key Properties

• CAS Number: 496794-70-8
• MW: 450.92
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₃ClN₄O₃
• SMILES: C(=O)(c1cc(cc(c1)OC)OC)Nc1cc(c(cc1)Cl)c1nc2c([nH]1)cc(cc2)N(C)C
• Target: TRP/TRPV Channel
• Solubility: DMSO : ≥ 100 mg/mL. 221.77 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  HhAntag (oral administraion; 75 mg/kg or 100 mg/kg; twice daily; 25 days) results in significant growth delay in HT55 and HT-29 colorectal cell line xenografts models, with average tumour growth inhibitions of 29% and 48%, respectively. Whereas HhAntag had no effect on the growth of DLD-1 xenografts. Animal model: Primary human xenografts in female CD1 nu/nu mice of 6–8 weeks (DLD-1, HT55 and HT-29 cells). Dosage: 75 mg/kg or 100 mg/kg. Administration: Oral administraion; twice daily; 25 days. Result: Resulted in growth delay of HT55 and HT-29 xenografts, but had no effects on DLD-1 xenografts.
• In Vitro:
  HhAntag (2-30 μM; 72 hours) demonstrates to be 10-times more potent than the natural product SMO antagonist, cyclopamine, at inhibiting Hh pathway activity and it inhibits Hh signalling pathway sensitivitive cells with IC50 values ranging from 2 μM to >30 μM. HhAntag inhibits AsPC-1, BXPC-3, CFPAC, HPAC, HPAF-II, KP4, Panc 03.27, PA-TU-8902, PSN-1, SU.86.86 cells with IC50 values of 30 μM, 5.4 μM, 5.8 μM, 2.7 μM, 6.2 μM, 10.3 μM, 2.5 μM, 2.9 μM, 5.8 μM and 2.7 μM, respectively. HhAntag (100 nM) is needed to completely inhibit Hh signalling in a Hh-responsive human mesenchymal cell line (HEPM) expressing a GLI luciferase reporter construct (HEPM-rep), the IC50 of 5 nM 400-times lower than that required to inhibit cell growth by 50% in the most sensitive cancer cell line (1.9 μM).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HhAntag | Hh-Antag | Hh Antag

Quick Database Links

Gene Symbol

TRP/TRPV Channel