HC278
HC278 is a selective TEAD1/TEAD3 PROTAC degrader. HC278 induces proteasome-dependent degradation by forming a stable ternary complex with CRBN/DDB1. HC278 is applicable to the research of mesothelioma.
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- CAS No.: 3096503-40-8
- Formule: C43H39F3N6O5
- Masse moléculaire:776.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
HC278 (50-500 nM; 2-18 h) is a bona fide, proteasome- and CRBN-dependent PROTAC that potently and selectively degrades TEAD1 and TEAD3 in HEK293 stable cells expressing epitope-tagged TEAD1-4, with significant degradation observed at 50 nM, while having minimal effect on TEAD2 and weak activity against TEAD4 at 500 nM[1].
HC278 (100-200 nM; two weeks) specifically inhibits the colony-forming ability of YAP-dependent NCI-H226 mesothelioma cells at 200 nM, while having no effect on NCI-H28 control mesothelioma cells[1].
HC278 (500 nM; 24 h) inhibits TEAD/YAP transcriptional activity in NCI-H226 mesothelioma cells, significantly downregulating YAP signature genes and specific target genes including CTGF, CYR61, and ANKRD1 at 500 nM for 24 h[1].
HC278 (500 nM-1 μM; 24 h) downregulates YAP target gene expression (CTGF, CYR61, ANKRD1) in MDA-MB-231 cells at 500 nM and 1 μM for 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 stable cells expressing epitope-tagged TEAD1-4 (FLAG-TEAD1, MYC-TEAD2, V5-TEAD3, HA-TEAD4)
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Concentration:50 nM; 500 nM
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Incubation Time:2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 14 h, 16 h, 18 h
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Result:Degraded TEAD1 and TEAD3 by more than 50% at 50 nM.
Had little effect on TEAD2, and only a weak degrading effect on TEAD4 at 500 nM.
Detected TEAD1/3 degradation as early as 2 h after treatment, with degradation increasing over time.
Completely blocked TEAD degradation when co-treated with 1 μM MG132.
Inhibited TEAD degradation activity when co-treated with 500 nM Ex.
29.
Showed much weaker degradative effect for negative control HC278-Neg1, and failed to induce TEAD degradation for negative control HC278-Neg2.
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Cell Line:NCI-H226 mesothelioma cells, NCI-H28 control mesothelioma cells
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Concentration:100 nM; 200 nM
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Incubation Time:two weeks
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Result:Significantly inhibited the colony-forming ability of NCI-H226 cells (YAP-dependent, NF2-deleted) at 200 nM, with little effect at 100 nM.
Had no apparent effect on the colony-forming ability of NCI-H28 cells (control, no Hippo pathway mutations) even at 200 nM.
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Cell Line:MDA-MB-231 cells
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Concentration:500 nM; 1 μM
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Incubation Time:24 h
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Result:Significantly downregulated the mRNA levels of YAP target genes CTGF, CYR61, and ANKRD1 compared to DMSO-treated cells.
Chemical Information
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CAS No. 3096503-40-8
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Masse moléculaire 776.80
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Formule C43H39F3N6O5
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SMILES
O=C1C2=CC=C(N3CCN(CC3)CC4=CC=CC([C@H](C)NC(C5=CC6=C(C(OC7=CC=C(C=C7)C(F)(F)F)=CC=C6)C=C5)=O)=N4)C=C2CN1C8C(NC(CC8)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HC278 Related Classifications
HY-185230 Related Classifications
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