Description
TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.
Product information
CAS Number: 2378626-29-8
Molecular Weight: 313.70
Formula: C15H11ClF3NO
Chemical Name: 2-chloro-1-(2-{[3-(trifluoromethyl)phenyl]amino}phenyl)ethan-1-one
Smiles: O=C(CCl)C1=CC=CC=C1NC1=CC(=CC=C1)C(F)(F)F
InChiKey: JPVDFGYNLUBCSD-UHFFFAOYSA-N
InChi: InChI=1S/C15H11ClF3NO/c16-9-14(21)12-6-1-2-7-13(12)20-11-5-3-4-10(8-11)15(17,18)19/h1-8,20H,9H2
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (318.78 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
TED-347 (0.5-100 μM; 48 hours) inhibits GBM43 cancer cell viability. TED-347 (5 μM; 48 hours) inhibits co-immunoprecipitation of Myc-tagged TEAD4 with FLAG-tagged Yap1. TED-347 (10 μM; 48 hours) shows a significant reduction in CTGF transcript levels. TED-347 (0.5-100 μM; 24 hours) reduces reporter activity in cells transfected with a TEAD reporter. TED-347 (0.5-100 μM) also inhibits TEAD4 transcriptional activity in GBM43 cells. TED-347 is selective for TEADs and inhibits TEAD2 with the same efficacy. TED-347 (0.1-100 μM; 24-48 hours) inhibits TEAD4 binding to full-length Yap1 in dose- and time-dependent manner. TED-347 (1-100 μM) shows no inhibition of uPAR•uPA or Cav2.2 α•β protein-protein interactions. Non-covalent binding of TED-347 to TEAD4 exhibits little change to the TEAD4•Yap1 binding affinity. TED-347 has the maximum rate of inactivation of 0.038 hours, corresponding to a t1/2∞ of 18.2 hours.
Products are for research use only. Not for human use.
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