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  4. OPN-9643

OPN-9643 is a covalent inhibitor targeting the central palmitate binding pocket of TEADs with an IC50 of 15 nM, preventing autopalmitoylation and reducing TEAD-driven luciferase activity and canonical TEAD targets, CTGF and CYR61. OPN-9643 can be used for the research of cancer, such as melanoma.

For research use only. We do not sell to patients.

OPN-9643

OPN-9643 Chemical Structure

CAS No. : 2866423-06-3

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OPN-9643 Related Antibodies

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Description

OPN-9643 is a covalent inhibitor targeting the central palmitate binding pocket of TEADs with an IC50 of 15 nM, preventing autopalmitoylation and reducing TEAD-driven luciferase activity and canonical TEAD targets, CTGF and CYR61. OPN-9643 can be used for the research of cancer, such as melanoma[1].

IC50 & Target.
[1]

TEAD

15 nM (IC50)

In Vitro

OPN-9643 (2 µM; 24-48 h) reduces the expression of TEAD targets (CTGF and CYR61) in SOX10 KO cells. OPN-9643 reduces luciferase activity. OPN-9643 reduces other known TEAD targets, such as DKK1, MYC, and TGF-β2 in SOX10 KO melanoma cells[1].\nOPN-9643 (NCI-H226 cells; 5 days) inhibits TEAD activity and cell growth (IC50 of 123 nM) in NCI-H226 cells[1].
When administered in combination with BRAFi (BRAF inhibitor) + MEKi (MEK inhibitor), and OPN-9643 (2 μM; 48-72 h) markedly decreases cell growth in A375 SOX10 KO cells compared to BRAFi + MEKi alone[1].
OPN-9643 (2 μM; 48 h) increases the cleaved-PARP and cleaved-GSDME in the combination treated SOX10 KO cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

OPN-9643 Related Antibodies

Western Blot Analysis[1]

Cell Line: A375 parental, A375 crSOX10 #2.18, and A375 crSOX10 #4.21 cells  
Concentration: 2 μM
Incubation Time: 24 h, 48 h
Result: Western blotting analysis detected a reduction in CTGF and CYR61 protein expression in SOX10 KO cells. 
Down-regulated the cell cycle progression regulators (FOXM1 and PLK1), growth factor receptors (phospho-cMET Y1234/5, AXL), a serine protease inhibitor (PAI1), and RAD51. 
Molecular Weight

347.33

Formula

C19H16F3NO2
CAS No.
SMILES

C=CC(N1CC2=C(C=CC(OC3=CC=C(C(F)(F)F)C=C3)=C2)CC1)=O
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Purity & Documentation
References
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OPN-9643 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OPN-96432866423-06-3OPN9643OPN 9643YAPYes-associated proteinactive TAZCYR61MEK inhibitorsMAPK-targeted therapiesTEAD targetsCTGFTEAD-dependent reporter activitySOX10 knockout cellscovalent inhibitorsBRAF inhibitorsacquired resistanceInhibitorinhibitorinhibit

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