MRT-92 is a potent selective Smoothened (Smo) receptor antagonist (Kd=0.3 nM), inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation with IC50 of 0.4 nM.

INS018_055 (INS018-055) a selective small-molecule TRAF2- and NCK-interacting kinase (TNIK) inhibitor with Kd value of 4.32 nM and IC50 of 31 nM, inhibits TGF-β-induced α-SMA protein expression in MRC-5 cells with IC50 of 27.14 nM.

C644-0303 is a novel Wnt/β-catenin signaling inhibitor (IC50=4.2 uM) with antitumor efficacy, inhibits both constitutive and ligand activated Wnt signals and its downstream gene expression.

ISQ-1 is a potent in vitro inhibitor of several cancer cell lines (LS174T cell proliferation, IC50=100 nM), inhibits Wnt signaling and also activates adenosine monophosphate kinase (AMPK).

LPD-01 is a small molecule inhibitor of the Wnt/β-catenin signaling pathway, directly binds to importin7, inhibits the transactivation of target genes of the Wnt/β-catenin signaling pathway.

WNTinib is a multi-kinase inhibitor with specificity against β-catenin (CTNNB1) mutant hepatocellular carcinoma, harnesses the KIT/MAPK/EZH2 pathway, shows durable and selective transcriptional repression of mutant β-catenin/Wnt targets through nuclear tr

A potent, selective γ-secretase inhibitor that significantly reduces the right ventricular systolic pressure and right heart hypertrophy in hypoxia/SU5416 (SUHx) rats..

RXC004 (RXC-004) is a potent, selective Porcupine (PRCN) inhibitor, inhibits functional Wnt production from mouse L-Wnt3a cells with IC50 of 64 pM in luciferase reporters assays.

WHN-88 is a potent, selective Porcupine (PORCN) inhibitor, inhibits Wnt/β-catenin signaling with IC50 of ST-Luc of 0.02 uM.

ZD06519 is a novel camptothecin payload for antibody drug conjugates (ADCs) with highp ayload potency (~1 nM).

A drug-linker conjugate for antibody-drug conjugate by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide SuO-Val-Cit-PAB..

EN106 derivative 1 is a EN106 derivative used for PROTAC design, EN106 is a covalent ligand and recruiter for FEM1B E3 ligase for targeted protein degradation.

EN106 derivative 2 is a EN106 derivative used for PROTAC design, EN106 is a covalent ligand and recruiter for FEM1B E3 ligase for targeted protein degradation.

Thalidomide-O-PEG4-Acid is a chemical linker for PROTAC design.

(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.

ARD-1676 (ARD1676) is a highly potent and orally efficacious PROTAC degrader of the androgen receptor (AR) with DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, respectively.

BI 1810284 (ACBI2, BI 01810284) is a potent, selective and orally bioavailable VHL-recruiting PROTAC degrader of SMARCA2 (DC50=1 nM in RKO cells), 30-fold selectivity over SMARCA4.

BJG-05-039 is a PAK1-selective degrader consisting of NVS-PAK1-1 conjugated to lenalidomide, a recruiter of the E3 ubiquitin ligase substrate adaptor Cereblon.

BSJ-04-146 is a potent, selective FAK PROTAC (IC50=26 nM), induces potent and durable FAK degradation in pancreatic and breast cancer cell lines at 10 nM.

BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78.

BTX-6654 is a potent, selective SOS1 cereblon-based bifunctional PROTAC degrader, reduces downstream signaling markers, pERK and pS6, and displayed antiproliferative activity in cells harboring various KRAS mutations.

BWA-522 is a potent, orally bioavailable PROTAC degrader of the androgen receptor N-terminal domain (AR-NTD), induces AR-FL or AR-V7 protein degradationwith DC50 of 0.73 μM (AR-FL) and 0.67 μM (AR-V7) in VCaP cells.