| DC70423 |
GA-017
|
GA-017 (GA017) is a potent, selective, ATP-competitive LATS kinase (LATS1/2) inhibitor with IC50 of 4.10/3.92 nM, respectively, promotes cell growth.GA-017 increases the number and size of spheroids of various cell-types in both scaffold-based and scaffold-independent cultures.GA-017 also enhances the ex vivo formation of mouse intestinal organoids.GA-017 facilitates the growth of spheroids and organoids by stabilizing and translocating YAP/TAZ into the cell nucleus.GA-017 inhibits the Hippo pathway to promote YAP/TAZ stabilization and nuclear translocation.GA-017 induces expression of Hippo pathway-related genes such as ANKRD1, CYR61, and CTGF in SKOV3 cells in a time- and dose-dependent manner.GA-017 inhibited the activity of 16 kinases of the AGC family at 100 nM against a panel of 321 diverse kinases.The serine/threonine protein kinases LATS (LATS1/2) phosphorylate YAP/TAZ, key effectors of the growth- and proliferation-regulating Hippo signaling pathway. |
| DC74457 |
UNC-SOB-5-16
|
UNC-SOB-5-16 is a potent, selective STK3 small-molecule inhibitor with IC50 of 22 nM, also inhibits LRRK2. |
| DC74456 |
UNC-BE4-017
|
UNC-BE4-017 is a selective STK3 small-molecule inhibitor, also potently inhibits JAK1, JAK2, and JAK3, but not other kinases in a panel of 48 kinases. |
| DC74455 |
TRULI
|
TRULI is a small molecule Yap signaling activator, acts as an ATP-competitive inhibitor of Lats kinases in vitro (Lats1 kinase, IC50=0.2 nM, 10 uM ATP), prevents Yap phosphorylation in the cell-based assays with EC50 of 510 nM. |
| DC74454 |
aNDR1
|
aNDR1 (NDR1 agonist) is a specific small-molecule agonist of Nuclear Dbf2-related kinase 1 (NDR1, STK38), specifically inhibits CRPC cells and promotes kinase activity of NDR1. |
| DC72123 |
IHMT-MST1-58
|
IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with IC50 value of 23 nM. IHMT-MST1-58 can be used for the research of Type 1/2 diabetes. |
| DC70888 |
VT02956
|
VT02956 is a potent, specific inhibitor of Hippo pathway kinase LATS with IC50 of 0.76 nM (LATS1) and 0.52 nM (LATS2), respectively;
VT02956 reduces YAP/TAZ phosphorylation in both dose- and time-dependent manner with IC50 of 0.16 μM and 0.43 μM in HEK293A cells and 4T1 cells, respectively.
VT02956 suppresses ESR1 transcription, dramaticly reduces ERα and its target genes TFF1 and GREB1.
VT02956 targets the LATS-YAP/TAZ-ERα axis to inhibit ER+ tumours cell growth, inhibits the proliferation of MCF-7 and T47D cells.
VT02956 inhibits the growth of T47D cells with hormone therapy resistant ESR1 mutation (ERa Y537S or D538G), enhances the anti-tumour effect of palbociclib in ER+ breast cancer cells. |
| DC70887 |
VT02484
|
VT02484 is the negative control compound of VT02956, which is a highly potent Hippo pathway kinase LATS inhibitor. |
| DC70834 |
TEAD-IN-2
|
TEAD-IN-2 (TEAD antagonist 2) is a small molecule TEAD antagonist (TEAD2 IC50=603 nM FP assays, SPR Kd=229 nM) that binds the TEAD lipid pocket and disrupts TEAD S-palmitoylation;
TEAD-IN-2 showed similar IC50 against all TEAD paralogs TEAD1, TEAD3, and TEAD4 both in IP and SRP assays.
TEAD-IN-2 disrupted Hippo signaling in a Detroit X1 562 cell reporter assay with IC50 of 31.8 nM, with no significant cytotoxicity indications in either primary human hepatocytes or human liver microtissues at 100 uM.
The inhibition of TEAD activity via TEAD-IN-2 was not due to the inability of TEAD to form a complex with YAP in cells.
TEAD-IN-2 functioned by acting as a TEAD S-palmitoylation mimic, binding and stabilizing newly translated TEAD proteins, TEAD-palmitoylation-deficient mutant K357A caused a stronger rescue of TEAD expression in HEK293T cells transfected TEAD2-K357A.
Dysregulating TEAD S-palmitoylation via TEAD-IN-2 could effectively inhibit Hippo-dependent tumor growth in vivo. |
