Products for Research Use Only

Pan-TEAD-IN-1

CAT: 0931-T203500-01Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0931-T203500-01Size:10 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
3027484-09-6
Target
YAP
Related Pathways
Stem Cells
Bioactivity
Pan-TEAD-IN-1 (Compound 3) is an orally active pan-inhibitor of TEAD, disrupting its interaction with coactivators YAP/TAZ by targeting the palmitoylation site of TEAD. This inhibition leads to the downregulation of oncogene transcription, such as Ctgf and Cyr61, within the Hippo signaling pathway. Demonstrating outstanding efficacy, pan-TEAD-IN-1 has an IC50 of 0.36 nM for luciferase and 1.52 nM for H226 cells, along with favorable pharmacokinetic properties (AUC0–∞= 228.7 μg/mL·min, T1/2= 183.9 min) . The compound significantly inhibits tumor growth in xenograft models of TEAD-dependent cancers, indicating its potential for research in these cancer types.
Smiles
O=C(C=C)N1CC=2C=C(C=CC2CC1)C3=CC=C(C=C3)C(F)(F)F
Molecular Formula
C19H16F3NO
Molecular Weight
331.33
Shipping Conditions
Ice Packs
Storage Temperature
-20°C