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Stem CellsYAP
YAP (Yes-associated protein) is a transcription co-activator in the Hippo tumor suppressor pathway and controls cell growth, tissue homeostasis and organ size. YAP is inhibited by the kinase Lats, which phosphorylates YAP to induce its cytoplasmic localization and proteasomal degradation. YAP induces gene expression by binding to the TEAD family transcription factors. The function of YAP in human cancer is complex and could be cell-type-dependent. For instance, YAP could function as a tumor suppressor in some cell types, such as hematological cancers, by inducing apoptosis in response to DNA damage.
- VerteporfinT3112129497-78-5Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.
- $34
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Cited - YAP-TEAD-IN-3T777252714434-21-4YAP-TEAD-IN-3 is an inhibitor of YAP/TAZ-TEAD interactions with an IC50 of 9 nM for Avi-human TEAD (4217-434). YAP-TEAD-IN-3 inhibits YAP reporter gene expression (IC50 = 0.048 μM) and NCI-H2052 cell proliferation (IC50 = 0.048 μM).
- $328
SizeQTY - VT104T678722417718-25-1VT104 is a potent and orally active YAP TAZ inhibitor for cancer research. VT104 blocks palmitoylation of endogenous TEAD1 and TEAD3 proteins.
- $72
SizeQTY - VT107T355452417718-63-7In houseVT107 is a potent pan-TEAD autopalmitoylation inhibitor. VT-107 can be used in cancer therapy research.[1]
- $147
SizeQTY - PY-60T95662765218-56-0PY-60 can effectively activate YAP transcriptional activity against annexin A2 (ANXA2) (Kd value of 1.4 µM). PY-60 activates a pro-proliferative, YAP-dependent transcriptional program in adult animals that are able to remodel the epidermis through proliferation.
- $116
SizeQTY - YAP-TEAD-IN-1 acetateTP2160L1YAP-TEAD-IN-1 acetate is an effective and competitive inhibitor of YAP–TEAD interaction with an IC50 of 25 nM.
- $147
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- AICART14772627-69-2AICAR (Acadesine) is an AMPK activator that causes ZMP accumulation, thereby mimicking the stimulatory effect of AMP on both AMPK and AMPKK. It is commonly used in research related to diabetes, cardiovascular diseases, and tumors.
- $30
SizeQTY Cited - Lats-IN-1T90531424635-83-5Lats-IN-1 is a potent and ATP-competitive Lats1 and Lats2 kinases inhibitor. It promotes Yap-dependent proliferation in postmitotic mammalian tissues.
- $67
SizeQTY Cited - IK-930T775802563892-44-2IK-930 is an orally active TEAD inhibitor (EC50 < 0.1 µM) with potent potency.
- $51
SizeQTY - MSC-4106T601482738542-58-8MSC-4106, an orally active and potent YAP TAZ-TEAD inhibitor, disrupts TEAD1 and TEAD3 auto-palmitoylation and demonstrates significant efficacy in the NCI-H226 tumor xenograft model [1].
- $97
SizeQTY - VT103T620772290608-13-6In houseVT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation and is an analog of VT101. VT103 has potential antitumor activity by inhibiting YAP TAZ-TEAD-promoted gene transcriptionment, blocking TEAD auto-palmitoylation, and blocking the interaction between YAP TAZ and TEAD.VT103 can be used in the study of HER2-positive breast cancer, prostate cancer, and triple-negative breast cancer.
- $126
SizeQTY - TT-10T697602230640-94-3TT-10 (TAZ-K), an activator of YES-associated protein (YAP)-transcriptional enhancer factor domain (TEAD) activity, has potential application in heart disease research, specifically for conditions characterized by loss of cardiomyocytes.
- $34
SizeQTY - YAP/TAZ inhibitor-2T602182762617-31-0YAP TAZ inhibitor-2 is a potent, orally active TEAD-YAP TAZ inhibitor with an EC50 value of 3 nM, demonstrating anti-proliferative and antitumor activity [1].
- $84
SizeQTY - TED-347T84212378626-29-8TED-347 is an irreversible and covalent inhibitor of TEAD4-Yap1 protein-protein interaction(EC50 of 5.9 μM), and inhibits glioblastoma cell viability.
- $78
SizeQTY - ML-7 hydrochlorideT3050110448-33-4ML-7 hydrochloride (ML-7 HCl) is a cell-permeable, reversible, effective, ATP-competitive, and specific inhibitor of myosin light chain kinase (Ki: 300 nM); also inhibits smooth-muscle myosin light chain kinase, PKA, and PKC.
- $30
SizeQTY Cited - GNE-7883T785582648450-42-2GNE-7883 is an inhibitor targeting TEAD transcription factor, inhibits cell proliferation and suppresses YAP/TAZ activation, and can be used to study YAP/TAZ-dependent tumors.
- $118
SizeQTY - YAP/TAZ inhibitor-1T133642093565-23-0YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor (IC50 <0.100 μΜ) for the study of abnormal immune function and cancer.
- $487
SizeQTY Cited - MY-1076T777293008262-76-5MY-1076 is a potent YAP inhibitor with antigastric cancer activity.MY-1076 dose-dependently induced G2/M phase block, induced YAP degradation and apoptosis, and inhibited microtubule protein polymerization.MY-1076 inhibited the proliferation of MGC-803, SGC-7901, HCT-116, and KYSE450 cells.
- $30
SizeQTY - MYF-01-37T223722416417-65-5MYF-01-37 (1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one) is a novel covalent TEAD inhibitor.
- $34
SizeQTY - AICAR phosphateT14149681006-28-0AICAR phosphate (Acadesine phosphate) is an AMPK activator and inhibitor of autophagy, YAP, and mitophagy. It serves as an adenosine analog, regulating glucose and lipid metabolism, and inhibiting the production of pro-inflammatory cytokines and iNOS.
- $49
SizeQTY - DC-TEADin02T643422380228-45-3DC-TEADin02 is an inhibitor of TEAD auto palmitoylation (IC50 = 197 nM). DC-TEADin02 can be in studies about development, regeneration, and tissue homeostasis.
- $30
SizeQTY - TEAD-IN-6T796872821763-12-4TEAD-IN-6 (Example 11-1) is a TEAD modulator that inhibits the YAP1 TAZ-TEAD interaction and has applications in cancer research [1].
- $1,520
SizeQTY - AF-2112T79428AF-2112, a TEAD inhibitor derived from Flufenamic acid, significantly diminishes the expression of CTGF, Cyr61, Axl, and NF2.
- $323
SizeQTY - YAP-TEAD-IN-2T728882714432-83-2YAP-TEAD-IN-2 (compound 6) is a potent inhibitor of the YAP-TEAD protein-protein interaction (PPI), with an inhibitory concentration 50 (IC50) value of 2.7 nM [1].
- $1,970
SizeQTY - LM-41T79427LM-41, a Flufenamic acid-derived TEAD inhibitor, significantly reduces the expression of CTGF, Cyr61, Axl, and NF2, and inhibits the migration of human MDA-MB-231 breast cancer cells [1].
- $75
SizeQTY - SWTX-143T810562766575-48-6SWTX-143, a novel covalent inhibitor, specifically and irreversibly binds to the palmitoylation pocket of all four TEAD isoforms, inhibiting the transcriptional activity of the YAP/TAZ-TEAD complex and demonstrating antitumor activity [1].
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