K-975
CAS No. 2563855-03-6
K-975( —— )
Catalog No. M28980 CAS No. 2563855-03-6
K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
5MG | 147 | Get Quote |
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10MG | 237 | Get Quote |
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25MG | 475 | Get Quote |
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50MG | 672 | Get Quote |
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100MG | Get Quote | Get Quote |
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200MG | Get Quote | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameK-975
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NoteResearch use only, not for human use.
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Brief DescriptionK-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.
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DescriptionK-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.(In Vitro):K-975 inhibits the cell proliferation of NRF2-non-expressing malignant pleural mesothelioma (MPM) cell lines, protein-protein interaction (PPI) between Halo-TAZ and TEAD1/4 and Halo-YAP and endogenous TEAD1/4 in NCl-H226 cells and the reporter activity in NCl-H661/CTGF-Luc cells with the maximum of ~70%, at concentration of 0.1-10000 nM at 144 h and 24 h, respectively . K-975 decreases the expression of IGFBP3, CTGF and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCl-H226 cells .(In Vivo):K-975 (10-300 mg/kg; p.o. twice a day for 14 days) suppresses the growth of tumors via inhibiting TEAD-YAP1/TAZ signaling in MPM xenograft mouse models .
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In VitroK-975 (0.1-10000 nM; 144 h) inhibits the cell proliferation of NF2-non-expressing malignant pleural mesothelioma (MPM) cell lines.K-975 (10-10000 nM; 24 h) inhibits protein-protein interaction (PPI) between Halo-YAP and endogenous TEAD1/4 and Halo-TAZ and TEAD1/4 in NCI-H226 cells.K-975 (0.1-10000 nM; 24 h) strongly inhibits the reporter activity in NCI-H661/CTGF-Luc cells, with the maximum inhibition of ~70%, and does not inhibit the reporter activity in NCI-H661/NRF2-Luc cells.K-975 (1-10000 nM; 24 h) decreases the expressions of CTGF, IGFBP3, and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCI-H226 cells. Cell Proliferation Assay Cell Line:NF2-non-expressing MPM and NF2-expressing malignant MPM cells Concentration:0.1, 1, 10, 100, 1000, 10000 nM Incubation Time:144 hours Result:Had a stronger inhibitory effect against NF2-non-expressing cell lines than NF2-expressing cell lines.Inhibited the proliferation of MSTO-211H cells, an NF2-expressing cell line.Western Blot Analysis Cell Line:NCI-H226 cells Concentration:10, 100, 1000, 10000 nMIncubation Time:24 hoursResult:Inhibited TEAD1-YAP1 PPI and TEAD4-YAP1 PPI.Inhibited TEAD1-TAZ PPI and TEAD4-TAZ PPI.
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In VivoK-975 (10-300 mg/kg; p.o. twice a day for 14 days) inhibits the tumor growth by inhibiting YAP1/TAZ-TEAD signaling in MPM xenograft mouse models. Animal Model:Male SCID mice (5 weeks) injected with NCI-H226 or MSTO-211H cells Dosage:10, 30, 100, 300 mg/kg Administration:P.o. twice a day for 14 days Result:Exhibited strong anti-tumor effect in MPM s.c. xenograft mouse models.Decreased the expressions of CTGF, IGFBP3, and NPPB, and increased the expression of FBXO32 in the NCI-H226 xenograft model.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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Recptor——
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Research Area——
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Indication——
Chemical Information
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CAS Number2563855-03-6
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Formula Weight287.74
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Molecular FormulaC16H14ClNO2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 220 mg/mL (764.58 mM)
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SMILESCC1=CC=C(NC(=O)C=C)C=C1OC1=CC=C(Cl)C=C1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Fuller RW, Mason NR, Molloy BB. Structural relationships in the inhibition of [(3)H]serotonin binding to rat brain membranes in vitro by 1-phenyl-piperazines. Biochem Pharmacol. 1980 Mar 1;29(5):833-5.
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