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YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity .
YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
Yap1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Yap1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Yap1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Yap1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
YAP1 Human Pre-designed siRNA Set A contains three designed siRNAs for YAP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
YAP/TEAD-IN-1 (compound 4) is a potent YAP and TEAD inhibitor. YAP/TEAD-IN-1 shows antioxidant activity. YAP/TEAD-IN-1 shows antiproliferation activity for tumor cells. YAP/TEAD-IN-1 shows little cytotoxic activity for human normal cells .
YAP/TAZ inhibitor-4 (Compound 45) is an inhibitor of YAP/TAZ, exhibiting TEAD transcriptional activation inhibitory activity by suppressing the binding of YAP or TAZ to TEAD .
YAP-IN-1 (Compound (+)-1) is an autophagy (Autophagy) inhibitor targeting YAP1. YAP-IN-1 binds to the Hippo pathway transcription factor YAP1 with a Kd of 9.13 μM and induces its degradation via the chaperone-mediated autophagy (CMA) pathway. This process inhibits Rab7-mediated fusion of autophagosomes and lysosomes, thereby reducing overall autophagy levels without affecting lysosomal function. YAP-IN-1 holds promise for research in cancer (e.g., liver cancer, breast cancer, etc.) .
YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that inhibits the interaction between YAP/TAZ and TEAD. YAP/TAZ-TEAD-IN-2 suppresses the transcriptional activity of TEAD, with an IC50 of 1.2 nM. YAP/TAZ-TEAD-IN-2 inhibits YAP/TAZ-TEAD target genes expression (Cyr61, CTGF, AXL and Survivin) and breast cancer cell proliferation .
YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
IAG933 (YAP-TEAD-IN-3) is an orally available YAP/TAZ-TEAD inhibitor that has anti-tumor effects and promotes apoptosis. IAG933 YAP-TEAD-IN-3 inhibits Avi-human TEAD 4217-434, with an IC50 value of 9 nM .
Human YAP1 mRNA encodes the human Yes1 associated transcriptional regulator (YAP1) protein, a downstream nuclear effector of the Hippo signaling pathway which is involved in development, growth, repair, and homeostasis. YAP1 is known to play a role in the development and progression of multiple cancers as a transcriptional regulator of this signaling pathway and may function as a potential target for cancer treatment.
PROTAC YAP degrader-1 (compound YZ-6) is a PROTAC targeting YAP and also inhibits the nuclear localization of YAP. PROTAC YAP degrader-1 is composed of PROTAC target protein ligand NSC682769 (HY-168017) (red part) and E3 ubiquitin ligase ligand + Linker conjugate (R,S,R)-AHPC-PEG2-C2-boc (HY-168019) (blue+black part), in which the PROTAC Linker used is Acid-PEG2-C2-Boc (HY-140480) and the target protein ligand activity control is Demethyl-NSC682769 (HY-168018) [1] .
TAT-PDHPS1 is a YAP inhibitor composed of the endogenous peptide PDHPS1 and the cell-penetrating peptide sequence TAT. PDHPS1 binds to protein phosphatase 2 phosphatase activator (PTPA), an essential activator of protein phosphatase 2A (PP2A), leading to increased YAP phosphorylation, which inactivates YAP and suppresses the expression of its downstream target genes. TAT-PDHPS1 is potentially useful in ovarian cancer research .
TEAD-IN-1 (Compound 2) is potent TEAD autopalmitoylation inhibitor, with an IC50 of 603 nM. TEAD-IN-1 increases the interaction of TEAD and VGLL4. TEAD-IN-1 decreases the interaction of YAP and TEAD. TEAD-IN-1 can be used for the research of cancer .
Tubulin polymerization-IN-58 (Compound K18) is a tubulin polymerization inhibitor with an IC50 of 0.446 μM. Tubulin polymerization-IN-58 also induces the degradation of oncogenic protein YAP via the UPS pathway, thus can be used for cancer research .
MY-1076 is an inhibitor of YAP. MY-1076 induces YAP degradation and cell apoptosis. MY-1076 inhibits MGC-803, SGC-7901, HCT-116 and KYSE450 cells proliferation with IC50 s of 0.019, 0.017, 0.020 and 0.044 μM, respectively .
mCMY020 is a covalent inhibitor of TEAD. mCMY020 effectively reduces YAP (Yes-associated protein)-driven transcription and selectively slows the proliferation of Hippo-deficient cancer cells. mCMY020 can be used in cancer research .
EN171 is a covalent ligand that covalently targets both C38 and C96 on 14-3-3 to enhance 14-3-3 interactions with ERα, YAP and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity. EN171 can not only be used as a molecular glue to enhance native protein interactions but can also be used as a covalent 14-3-3 recruiter in heterobifunctional molecules to sequester nuclear neo-substrates such as BRD4 and BLC6 into the cytosol .
Tubulin polymerization-IN-79 (Compound C20) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-79 shows potent antiproliferative activity against esophageal cancer cells (e.g., KYSE450, IC50=0.36 μM; EC-109, IC50=0.63 μM). Tubulin polymerization-IN-79 occupies the colchicine binding site to disrupt microtubule network integrity, activating the Hippo signaling pathway, downregulating the oncogenic protein YAP expression, and inducing G2/M phase arrest and apoptosis in esophageal cancer cells. Tubulin polymerization-IN-79 is promising for research of esophageal cancers .
BAY-593 (hydrochloride) is an orally active GGTase-I inhibitor. BAY-593 (hydrochloride) can block YAP1/TAZ signaling in animals and has antitumor activity .
TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells .
TEAD-IN-9 (compound 17) is a TEAD1 inhibitor with an IC50 of 0.29 μM. TEAD-IN-9 targets the palmitoyl pocket of TEAD, thereby effectively inhibiting the binding of YAP-TEAD and blocking the transcriptional function of YAP-TEAD .
TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity .
SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity .
Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation .
PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity .
(7S)-BAY-593 is the S-enantiomer of BAY-593 (HY-161573). BAY-593 is an orally active GGTase-I inhibitor. BAY-593 can block YAP1/TAZ signaling in animals and has antitumor activity .
VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer .
Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis . Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation .
MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma .
Verteporfin (Standard) is the analytical standard of Verteporfin. This product is intended for research and analytical applications. Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis . Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation .
TRULI (Lats-IN-1) is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. TRULI promotes Yap-dependent proliferation in postmitotic mammalian tissues .
GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor .
NSC682769 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). NSC682769 can be used for synthesis PROTAC YAP degrader-1 (HY-168016) .
VT104 is a potent and orally active YAP/TAZ inhibitor. VT104 prevents palmitoylation of endogenous TEAD1 and TEAD3 proteins. VT104 can be used in research of cancer .
TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration .
MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206 + tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models .
Demethyl-NSC682769 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Demethyl-NSC682769 can be used in synthesis PROTAC YAP degrader-1 (HY-168016) .
TT-10 (TAZ-K) is an activator of YES-associated protein (YAP)-transcriptional enhancer factor domain (TEAD) activity. TT-10 can be used for the research of heart diseases accompanied by cardiomyocyte loss .
MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .
Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR is also an autophagy, YAP and mitophagy inhibitor. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR inhibits autophagy through a mechanism independent of AMPK activity .
AICAR (phosphate) (Standard) is the analytical standard of AICAR (phosphate). This product is intended for research and analytical applications. AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor .
NIBR-LTSi is an orally active and selective LATS kinase inhibitor. NIBR-LTSi can activate YAP signaling. NIBR-LTSi promotes stem cell proliferation, maintains stemness and blocks differentiation. NIBR-LTSi accelerates liver regeneration following extended hepatectomy in mice .
AICAR (Standard) is the analytical standard of AICAR. This product is intended for research and analytical applications. AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
KHKI-01215 is an inhibitor for NUAK2 with an IC50 of 0.052 μM. KHKI-01215 inhibits the proliferation of cancer cell SW480 with an IC50 of 3.16 μM, induces apoptosis in SW480. KHKI-01215 inhibits the YAP signaling pathway .
Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
HDAC11-IN-1 (Compound 14-N C6OH) is a selective macrocyclic inhibitor of HDAC11 with a Ki of 40 nM. HDAC11-IN-1 exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2 .
HDAC11-IN-1 (Compound 14-N C6OH) TFA is a selective macrocyclic inhibitor of HDAC11 with a Ki of 40 nM. HDAC11-IN-1 TFA exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2 .
α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
Lappaol F, a lignin, is an anticancer agent. Lappaol F inhibits YAP mRNA and protein level. Lappaol F inhibits tumor cell growth by inducing cell cycle arrest. Lappaol F induces cancer cell apoptosis, and inhibits tumor growth. Lappaol F can be isolated from Arctium lappa Linne (Asteraceae) .
Pipecolic acid-d9 is the deuterium labeled Pipecolic acid. Pipecolic acid is a metabolite of lysine and an important precursor for many useful microbial secondary metabolites. Pipecolic acid slows ferroptosis in diabetic retinopathy by inhibiting the YAP-GPX4 signaling pathway. In addition, Pipecolic acid can be used as a diagnostic marker for pyridoxine-dependent epilepsy .
N-Acetylgalactosaminyltransferase 12 (GALNT12) belongs to the uridine diphosphate N-acetylgalactosamine gene family and is involved in the biological processes of many diseases, such as tumor progression. N-Acetylgalactosaminyltransferase 12 is a potential biomarker for fibrosarcoma, and its high expression level is closely related to the yes1-associated transcriptional regulator (YAP1) signaling pathway .
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(S,R,S)-AHPC-PEG2-C2-boc is an E3 Ligase Ligand-Linker Conjugate. (S,R,S)-AHPC-PEG2-C2-boc can be used to synthesize PROTAC YAP degrader-1 (HY-168016) .
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity . Dihydrexidine can stimulate YAP phosphorylation .
Pipecolic acid (Standard) is the analytical standard of Pipecolic acid. This product is intended for research and analytical applications. Pipecolic acid is a metabolite of lysine and an important precursor for many useful microbial secondary metabolites. Pipecolic acid slows ferroptosis in diabetic retinopathy by inhibiting the YAP-GPX4 signaling pathway. In addition, Pipecolic acid can be used as a diagnostic marker for pyridoxine-dependent epilepsy .
Pipecolic acid is a metabolite of lysine and an immunomodulator, which can induce systemic acquired resistance (SAR) in plants. Pipecolic acid inhibits ferroptosis in diabetic retinopathy through the YAP-GPX4 signaling pathway. Pipecolic acid can induce apoptosis in neuronal cells. In addition, Pipecolic acid can be used as a diagnostic marker for pyridoxin-dependent epilepsy .
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity . Dihydrexidine hydrochloride can stimulate YAP phosphorylation .
HTH-02-006 is a NUAK2 inhibitor (IC50=126 nM). HTH-02-006 reduces levels of phosphorylated MYPT1 in HuCCT-1 cells. HTH-02-006 inhibits YAP-driven cell proliferation, hepatomegaly and tumorigenesis. HTH-02-006 also has antifibrotic protective effect .
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
TD034 is a selective, reversible and noncovalent HDAC11 inhibitor with an IC50 of 5.1 nM and a Ki of 1.5 nM. TD034 does not inhibit other HDACs or sirtuins. TD034 inhibits the defatty acylation of SHMT2 (HDAC11 substrate). TD034 decreases the YAP1 level via HDAC11 inhibition. TD034 can be used for the study of lung cancer .
AICAR- 13C2, 15N (Acadesine- 13C2, 15N; AICA Riboside- 13C2, 15N) is the 13C and 15N labeled AICAR (HY-13417) . AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
M3686 (Compound 29) is a potent, selective TEAD1 inhibitor with an IC50 value of 51 nM. M3686 also shows weaker binding activity on TEAD3. M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with an IC50 value of 0.06 uM. M3686 shows strong anti-tumor effects in the NCI-H226 xenograft model .
PY-PAP is a photoactivatable affinity probe and a derivative of PY-60 (HY-141644). PY-PAP retains the cellular function of activating YAP transcriptional activity. In 293A cells, PY-PAP can label cathepsin D (CTSD) and annexin A2 (ANXA2) through ultraviolet crosslinking and click reactions. PY-PAP plays a key role in identifying ANXA2 as the specific target of PY-60 .
α-Ionone (Standard) is the analytical standard of α-Ionone. This product is intended for research and analytical applications. α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
CV-4-26 (Compound 22) is a covalent inhibitor of TEAD. CV-4-26 inhibits YAP/TEAD-based transcription, leading to the reduction of CTGF and CYR61 expression. CV-4-26 inhibits Huh7 and HepG2 cell colony formation, induces cell cycle arrest, and apoptosis. CV-4-26 shows antitumor activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB) .
Flufenamic acid (Standard) is the analytical standard of Flufenamic acid. This product is intended for research and analytical applications. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
Flufenamic acid- 13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK . Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells .
GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC50 values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids .
Cytochalasin D (Zygosporin A) is a potent actin polymerization inhibitor, could be derived from fungus. Cytochalasin D has cell-permeable activity. Cytochalasin D inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells. Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of Yap .
Ki16425 (Standard) is the analytical standard of Ki16425. This product is intended for research and analytical applications. Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK . Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells .
USP10-IN-4 is a potent ubiquitin-specific protease 10 (USP10) inhibitor with an IC50 of 10.87 μM and a Kd of 365 nM. USP10-IN-4 effectively inhibits USP10-mediated proteasomal degradation of downstream proteins YAP and p53, leading to the subsequent downregulation of CDK4 in the p53 signaling pathway. USP10-IN-4 promotes apoptosis in HCC cells and inhibits the onset and progression of liver cancer. USP10-IN-4 can used for the study of hepatocellular carcinoma (HCC) .
Chikusetsusaponin IVa is an orally active protein kinase activator. Chikusetsusaponin IVa binds to YAP with a KD value of 0.388 mM. Chikusetsusaponin IVa reduces inflammatory mediators (IL-6, IL-10, COX-2) expression, NO production, promotes ROS generation, induces Apoptosis, inhibits MAPK, TAZ, and regulates Nrf2, JAK/STAT. Chikusetsusaponin Iva has anti-H9N2 AIV and anti-endometrial cancer activities. Chikusetsusaponin Iva shows anti-inflammatory, hepatoprotective and osteoprotective effects .
LY294002 (Standard) is the analytical standard of LY294002. This product is intended for research and analytical applications. LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively . LY294002 also inhibits CK2 with an IC50 of 98 nM . LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4?μM. LY294002 is an apoptosis activator .
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively . LY294002 also inhibits CK2 with an IC50 of 98 nM . LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator .
PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293T cells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383))
Acid Ceramidase-IN-3 is a acid ceramidase (aCDase) inhibitor. Acid Ceramidase-IN-3 inhibits the enzymatic activity of aCDase with a pIC 50 of 8.5 in enzymatic assays and 6.8 in A375 melanoma cellular assays. Acid Ceramidase-IN-3 promotes HSC inactivation, as measured by a dose-dependent
reduction in COL1A1 and ACTA2. Acid Ceramidase-IN-3 inhibits aCDase activity in HSCs, promotes HSC inactivation and suppresses YAP/TAZ nuclear localization. Acid Ceramidase-IN-3 increases Dynein/Kinesin (NDE1, NDEL1.
KIF3B, KIF15) while decreases several proteins involved with signaling pathway (SARM1, RGAP1,
PDGF-D,PDGFR-B). Acid Ceramidase-IN-3 can be used for the study of fibrotic diseases .
pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
Pipecolic acid (Standard) is the analytical standard of Pipecolic acid. This product is intended for research and analytical applications. Pipecolic acid is a metabolite of lysine and an important precursor for many useful microbial secondary metabolites. Pipecolic acid slows ferroptosis in diabetic retinopathy by inhibiting the YAP-GPX4 signaling pathway. In addition, Pipecolic acid can be used as a diagnostic marker for pyridoxine-dependent epilepsy .
Pipecolic acid is a metabolite of lysine and an immunomodulator, which can induce systemic acquired resistance (SAR) in plants. Pipecolic acid inhibits ferroptosis in diabetic retinopathy through the YAP-GPX4 signaling pathway. Pipecolic acid can induce apoptosis in neuronal cells. In addition, Pipecolic acid can be used as a diagnostic marker for pyridoxin-dependent epilepsy .
YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation .
Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
TAT-PDHPS1 is a YAP inhibitor composed of the endogenous peptide PDHPS1 and the cell-penetrating peptide sequence TAT. PDHPS1 binds to protein phosphatase 2 phosphatase activator (PTPA), an essential activator of protein phosphatase 2A (PP2A), leading to increased YAP phosphorylation, which inactivates YAP and suppresses the expression of its downstream target genes. TAT-PDHPS1 is potentially useful in ovarian cancer research .
MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206 + tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models .
Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation .
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor .
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR is also an autophagy, YAP and mitophagy inhibitor. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR inhibits autophagy through a mechanism independent of AMPK activity .
AICAR (Standard) is the analytical standard of AICAR. This product is intended for research and analytical applications. AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
Cytochalasin D (Zygosporin A) is a potent actin polymerization inhibitor, could be derived from fungus. Cytochalasin D has cell-permeable activity. Cytochalasin D inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells. Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of Yap .
Chikusetsusaponin IVa is an orally active protein kinase activator. Chikusetsusaponin IVa binds to YAP with a KD value of 0.388 mM. Chikusetsusaponin IVa reduces inflammatory mediators (IL-6, IL-10, COX-2) expression, NO production, promotes ROS generation, induces Apoptosis, inhibits MAPK, TAZ, and regulates Nrf2, JAK/STAT. Chikusetsusaponin Iva has anti-H9N2 AIV and anti-endometrial cancer activities. Chikusetsusaponin Iva shows anti-inflammatory, hepatoprotective and osteoprotective effects .
AICAR (phosphate) (Standard) is the analytical standard of AICAR (phosphate). This product is intended for research and analytical applications. AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor .
Lappaol F, a lignin, is an anticancer agent. Lappaol F inhibits YAP mRNA and protein level. Lappaol F inhibits tumor cell growth by inducing cell cycle arrest. Lappaol F induces cancer cell apoptosis, and inhibits tumor growth. Lappaol F can be isolated from Arctium lappa Linne (Asteraceae) .
α-Ionone (Standard) is the analytical standard of α-Ionone. This product is intended for research and analytical applications. α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
YAP1 is a multifunctional transcriptional regulator and an important downstream target in the Hippo signaling pathway, affecting organ size control and tumor suppression through proliferation and apoptosis regulation. STK3/MST2 and STK4/MST1 phosphorylate together with SAV1, inactivating YAP1 and WWTR1/TAZ oncoproteins. YAP1 Protein, Human (His) is the recombinant human-derived YAP1 protein, expressed by E. coli, with C-10*His labeled tag.
Pipecolic acid-d9 is the deuterium labeled Pipecolic acid. Pipecolic acid is a metabolite of lysine and an important precursor for many useful microbial secondary metabolites. Pipecolic acid slows ferroptosis in diabetic retinopathy by inhibiting the YAP-GPX4 signaling pathway. In addition, Pipecolic acid can be used as a diagnostic marker for pyridoxine-dependent epilepsy .
Flufenamic acid- 13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
AICAR- 13C2, 15N (Acadesine- 13C2, 15N; AICA Riboside- 13C2, 15N) is the 13C and 15N labeled AICAR (HY-13417) . AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
YAP1 Antibody (YA4039) is a mouse-derived and non-conjugated IgG1 antibody, targeting to YAP1. It can be applicated for WB, IHC-P, FC, ELISA assays, in the background of human, mouse, rat, monkey, rabbit.
YAP1 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 54 kDa, targeting to YAP1. It can be used for WB,ICC/IF,IHC-P,IP,FC assays with tag free, in the background of Human.
Phospho-YAP1 (Ser127) Antibody (YA137) is a non-conjugated and Rabbit origined monoclonal antibody about 54 kDa, targeting to Phospho-YAP1 (S127). It can be used for WB,IHC-P assays with tag free, in the background of Human, Mouse.
Phospho-YAP(Ser127) Antibody (YA5859) is a rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to phosphorylated YAP (Ser127). It can be applicated for WB, ICC/IF, IP, ELISA assays, in the background of human, mouse, rat.
PY-PAP is a photoactivatable affinity probe and a derivative of PY-60 (HY-141644). PY-PAP retains the cellular function of activating YAP transcriptional activity. In 293A cells, PY-PAP can label cathepsin D (CTSD) and annexin A2 (ANXA2) through ultraviolet crosslinking and click reactions. PY-PAP plays a key role in identifying ANXA2 as the specific target of PY-60 .
Yap1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Yap1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Yap1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Yap1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
YAP1 Human Pre-designed siRNA Set A contains three designed siRNAs for YAP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Human YAP1 mRNA encodes the human Yes1 associated transcriptional regulator (YAP1) protein, a downstream nuclear effector of the Hippo signaling pathway which is involved in development, growth, repair, and homeostasis. YAP1 is known to play a role in the development and progression of multiple cancers as a transcriptional regulator of this signaling pathway and may function as a potential target for cancer treatment.
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