IMR-1A is the metabolite of IMR-1. IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μmol/L.

IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis.

IC261 is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.

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

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

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

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.

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).

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.

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.

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.

AG-1031 (AG1031) is a specific small molecule inhibitor of the double-stranded DNA binding activity of positive coactivator 4 (PC4) with IC50 of 2.5 uM, more effectively than its single-stranded DNA binding activity (IC50=15 uM).

UNC-SOB-5-16 is a potent, selective STK3 small-molecule inhibitor with IC50 of 22 nM, also inhibits LRRK2.

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.

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.

Picoberin is a highly potent (low picomolar) inhibitor of purmorphamine- and Sonic Hedgehog (Shh)-induced osteogenesis with IC50 of 3 pM, acts as an AhR agonist and induces the expression of AhR target genes, thereby suppressing osteoblast differentiation

MDB5 is a potent hedgehog (Hh) signaling pathway inhibitor, exhibits stronger inhibition of the Hh pathway and anticancer effect in vitro and vivo than GDC-0449.

NPL-4011 is a specific small molecule inhibitor of PDZ domain of human Dvl1 (Dvl1-PDZ) with KD vaule of 34.5 uM in NMR titration experiments.

BMD4722 is a highly potent, small-molecule inhibitor of Dvl-CXXC5 interaction with IC50 of 2.59 uM, directly binds to the Dvl PDZ domain (Kd=22.3 uM).

BMD4702 is a small molecule Dishevelled (Dvl) PDZ domain with binding Kd of 186 nM.

SR-4133 (SR4133) is a potent and highly selective CK1ε isoform inhibitor with IC50 of 58 nM, no significant acitivity agianst CK1δ (IC50>10,000 nM).

SGC-CK2-1 analog 2h is potent, selective and in vivo active inhibitor of casein kinase 2α (CSNK2A, CK2α) with pIC50 of 7.5 and 7.7 against CSNK2A1 and CSNK2A2, respectively.

CKR-49-17 is a potent, allosteric small molecule activator of CK1γ2 with Kd value of 180 nM in MST assays.

AB668 is a selective, bivalent Casein Kinase 2 (CK2) inhibitor targeting the ATP site and the αD pocket, AB668 inhibits the CK2 holoenzyme with Ki value of 41 nM (IC50=65 nM).

IMU1003 (IMU-1003) is a small molecule inhibitor of Wnt/β-catenin signaling, decreases β-catenin levels and inhibits target gene expression that promotes cancer cell proliferation.

CW85319 is a small-molecule compound that enhances Axin2's interaction with GSK3β, shows a high-affinity binding with Axin2 with Kd of 5.8 uM.

PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.

KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.

CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).

Fosciclopirox suppresses growth of urothelial cancer by targeting the γ-secretase complex. Fosciclopirox selectively delivers the active metabolite, Ciclopirox (CPX), to the entire urinary tract. Ciclopirox has anticancer activity in a number of solid and hematologic malignancies.