hippo pathway

XMU-MP-1 is an inhibitor of the pro-apoptotic, sterile 20-like kinases MST1 and 2.

Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM 6 nM 8 nM 0.5 nM and 32 nM for JAK1 JAK2 JAK3 TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

IHMT-MST1-58 is a STE20-like protein 1 kinase (MST1) inhibitor (IC50:23 nM) with high efficiency, selectivity and oral activity. IHMT-MST1-58 can be used to study type 1 or type 2 diabetes.

Pim1 AKK1-IN-1 (LKB1 AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM 53 nM 75 nM 380 nM for Pim1 AKK1 MST2 LKB1 respectively, and also inhibits MPSK1 and TNIK.

I3MT-3 (HMPSNE) (HMPSNE) is a potent, selective and cell membrane permeability inhibitor of 3-mercaptopyruvate sulfur transferase (3MST), which targets the persulfated cysteine residues located at the active site of 3MST.

EN171, a covalent ligand, selectively binds to C38 and C96 on 14-3-3, intensifying 14-3-3's interactions with ERα, YAP, and TAZ. This action impairs both estrogen receptor and Hippo pathway transcriptional activities. Beyond serving as a molecular glue to augment native protein interactions, EN171 also functions as a covalent recruiter for 14-3-3 in heterobifunctional molecules. This facilitates the sequestration of nuclear neo-substrates, such as BRD4 and BLC6, into the cytosol.

pan-TEAD-IN-1 (Compound 3) is an orally active pan-inhibitor of TEAD, disrupting its interaction with coactivators YAP TAZ by targeting the palmitoylation site of TEAD. This inhibition leads to the downregulation of oncogene transcription, such as Ctgf and Cyr61, within the Hippo signaling pathway. Demonstrating outstanding efficacy, pan-TEAD-IN-1 has an IC50 of 0.36 nM for luciferase and 1.52 nM for H226 cells, along with favorable pharmacokinetic properties (AUC0–∞= 228.7 μg mL·min, T1 2= 183.9 min). The compound significantly inhibits tumor growth in xenograft models of TEAD-dependent cancers, indicating its potential for research in these cancer types.

MY-1576 is a FAK inhibitor with an IC50 of 8 nM. It activates the Hippo pathway, thereby inhibiting YAP TAZ regulation. Additionally, MY-1576 effectively suppresses tumor growth in the KYSE30 xenograft mouse model, demonstrates good safety, and efficiently downregulates FAK autophosphorylation and YAP TAZ levels in vivo.

MY-875 is a potent microtubulin polymerization inhibitor that competes at colchicine binding sites, exhibiting an IC50 value of 0.92 μM. It effectively suppresses microtubulin polymerization, exerting its inhibitory effect. Additionally, MY-875 exerts its biological impact by activating the Hippo pathway, inducing apoptosis, and displaying commendable anticancer activity [1].

VT02956 is a LATS inhibitor ( IC 50 : 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 .