YAP-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/YAP.html YAPYes-associated proteinYAP (Yes-associated protein) is a transcription co-activator in the Hippo tumor suppressor pathway and controls cell growth, tissuehomeostasis and organ size. YAP is inhibited by the kinase Lats, which phosphorylates YAP to ind

2、uce its cytoplasmic localizationand 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 tumorsuppressor in some cell types, such

3、 as hematological cancers, by inducing apoptosis in response to DNA damage.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/YAP.html YAP HYPERLINK https:/www.MedChemE/Targets/YAP.html HYPERLINK https:/www.MedChemE/Targets/YAP.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/YAP.html HYPERL

4、INK https:/www.MedChemE/Targets/YAP.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/YAP.html HYPERLINK https:/www.MedChemE/Targets/YAP.html Activators HYPERLINK https:/www.MedChemE/Targets/YAP.html HYPERLINK https:/www.MedChemE/Targets/YAP.html & HYPERLINK https:/www.MedChemE/Targets/YAP.htm

5、l HYPERLINK https:/www.MedChemE/Targets/YAP.html Modulators HYPERLINK https:/www.MedChemE/AICAR.html AICAR(Acadesine; AICA Riboside) Cat. No.: HY-13417 HYPERLINK https:/www.MedChemE/AICAR-phosphate.html AICAR HYPERLINK https:/www.MedChemE/AICAR-phosphate.html HYPERLINK https:/www.MedChemE/AICAR-phos

6、phate.html phosphate(Acadesine phosphate; AICA Riboside phosphate) Cat. No.: HY-13417AAICAR (Acadesine) is an adenosine analog and aAMPK activator. AICAR regulates the glucose andlipid metabolism, and inhibits proinflammatorycytokines and iNOS production. AICAR is also anautophagy, YAP and mitophagy

7、 inhibitor.AICAR phosphate (Acadesine phosphate) is anadenosine analog and a AMPK activator. AICARphosphate regulates the glucose and lipidmetabolism, and inhibits proinflammatory cytokinesand iNOS production. AICAR phosphate is also anautophagy, YAP and mitophagy inhibitor.Purity: 99.92%Clinical Da

8、ta: Phase 3Size: 50 mg, 100 mg, 200 mg, 500 mgPurity: 99.49%Clinical Data: Phase 3Size: 10 mM 1 mL, 50 mg, 100 mg, 200 mg, 500 mg HYPERLINK https:/www.MedChemE/cytochalasin-d.html Cytochalasin HYPERLINK https:/www.MedChemE/cytochalasin-d.html HYPERLINK https:/www.MedChemE/cytochalasin-d.html D(Zygos

9、porin A; NSC 209835) Cat. No.: HY-N6682 HYPERLINK https:/www.MedChemE/k-975.html K-975Cat. No.: HY-138565Cytochalasin D (Zygosporin A; NSC 209835) is apotent and cell-permeable inhibitor of actinpolymerization derived from fungus, inhibits theG-actincofilin interaction by binding to G-actin.K-975 is

10、 a potent, selective and orally activeTEAD inhibitor, with a strong inhibitory effectagainst protein-protein interactions betweenYAP1/TAZ and TEAD. K-975 covalently binds toCys359 located in the palmitate-binding pocket ofTEAD via an acrylamide structure.Purity: 99.75%Clinical Data: No Development R

11、eportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 98.55%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/lats-in-1.html Lats-IN-1 HYPERLINK https:/www.MedChemE/lats-in-1.html HYPERLINK https:/www.MedChemE/ML-7-hydrochloride.html ML-7 HYPERLI

12、NK https:/www.MedChemE/ML-7-hydrochloride.html HYPERLINK https:/www.MedChemE/ML-7-hydrochloride.html hydrochlorideCat. No.: HY-138489 Cat. No.: HY-15417Lats-IN-1 is a potent and ATP-competitiveinhibitor of Lats1 and Lats2 kinases. Lats-IN-1promotes Yap-dependent proliferation inpostmitotic mammalian

13、 tissues.ML-7 hydrochloride is a naphthalene sulphonamidederivative, potently inhibits MLCK (IC =30050nM). ML-7 hydrochloride also inhibits YAP/TAZ.Purity: 99.98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.75%Clinical Data: No Development ReportedSize: 10

14、mM 1 mL, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/myf-01-37.html MYF-01-37 HYPERLINK https:/www.MedChemE/myf-01-37.html HYPERLINK https:/www.MedChemE/py-60.html PY-60Cat. No.: HY-139603 Cat. No.: HY-141644MYF-01-37 is a covalent TEAD inhibitor targetingCys380. MYF-01-37 has a reversible inhibition

15、 onYAP/TEAD interaction.PY-60 is a robust and specific activator of YAPtranscriptional activity that targets annexin A2(ANXA2) with a K of 1.4 M. PY-60 directlydbinds to ANXA2 and antagonizes its normal cellularfunction of repressing YAP activity.Purity: 98.98%Clinical Data: No Development ReportedS

16、ize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.63%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/super-tdu.html Super-TDU HYPERLINK https:/www.MedChemE/super-tdu.html HYPERLINK https:/www.MedChemE/super-tdu-1-31.html Super-TDU HYPER

17、LINK https:/www.MedChemE/super-tdu-1-31.html HYPERLINK https:/www.MedChemE/super-tdu-1-31.html (1-31)Cat. No.: HY-P1727 Cat. No.: HY-P1728Super-TDU is a specific YAP antagonist targetingYAP-TEADs interaction. Super-TDU suppresses tumorgrowth in gastric cancer mouse model.Super-TDU (1-31) is a peptid

18、e of Super-TDU, whichis an inhibitor of YAP-TEADs, shows potentanti-tumor activity.Purity: 98.85%Clinical Data: No Development ReportedSize: 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/

19、super-tdu-1-31-tfa.html Super-TDU HYPERLINK https:/www.MedChemE/super-tdu-1-31-tfa.html HYPERLINK https:/www.MedChemE/super-tdu-1-31-tfa.html (1-31) HYPERLINK https:/www.MedChemE/super-tdu-1-31-tfa.html HYPERLINK https:/www.MedChemE/super-tdu-1-31-tfa.html (TFA) HYPERLINK https:/www.MedChemE/super-t

20、du-1-31-tfa.html HYPERLINK https:/www.MedChemE/super-tdu-tfa.html Super-TDU HYPERLINK https:/www.MedChemE/super-tdu-tfa.html HYPERLINK https:/www.MedChemE/super-tdu-tfa.html TFACat. No.: HY-P1728A Cat. No.: HY-P1727ASuper-TDU (1-31) is a peptide of Super-TDU, whichis an inhibitor of YAP-TEADs, shows

21、 potentanti-tumor activity.Super-TDU TFA is a specific YAP antagonisttargeting YAP-TEADs interaction. Super-TDU TFAsuppresses tumor growth in gastric cancer mousemodel.Purity: 96.04%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPE

22、RLINK https:/www.MedChemE/ted-347.html TED-347Cat. No.: HY-125269 HYPERLINK https:/www.MedChemE/Verteporfin.html Verteporfin(CL 318952) Cat. No.: HY-B0146TED-347 is a potent, irreversible, covalent andallosteric inhibitor at YAP-TEAD protein-proteininteraction with an EC of 5.9 M for TEAD4Yap150prot

23、ein-protein interaction.Verteporfin (CL 318952) is a photosensitizer forphotodynamic therapy to eliminate the abnormalblood vessels in the eye associated withconditions such as age-related maculardegeneration. Verteporfin is a YAP inhibitorwhich disrupts YAP-TEAD interactions.Purity: 98.78%Clinical

24、Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.58%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/vt103.html VT103 HYPERLINK https:/www.MedChemE/vt103.html HYPERLINK https:/www.MedChemE/vt107.html VT107Cat. N

25、o.: HY-134955 Cat. No.: HY-134957VT103, an analog of VT101, is an orally active andselective TEAD1 protein palmitoylation inhibitor.VT103 inhibits YAP/TAZ-TEAD promoted genetranscription, blocks TEAD auto-palmitoylation,and disrupts interaction between YAP/TAZ andTEAD.VT-107, as an analogous to VT10

26、4, is an orallyactive and potent pan-TEAD auto-palmitoylationinhibitor. VT-107 can be used for the research ofcancer.Purity: 99.21%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.98%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50

27、 mg, 100 mg HYPERLINK https:/www.MedChemE/yap-tead.html YAP-TEAD-IN-1 HYPERLINK https:/www.MedChemE/yap-tead.html HYPERLINK https:/www.MedChemE/yap-tead-tfa.html YAP-TEAD-IN-1 HYPERLINK https:/www.MedChemE/yap-tead-tfa.html HYPERLINK https:/www.MedChemE/yap-tead-tfa.html TFACat. No.: HY-P2244 Cat. No.: HY-P2244AYAP-TEAD-IN-1 is a potent and competitiveinhibitor of YAPTEAD interaction (IC =2550nM). YAP-TEAD-IN-1 is a 17mer pep