NADI-351 is a specific small-molecule inhibitor of Notch1 transcriptional complexes with IC50 of 8.8 uM in cellualr reporter assays.NADI-351 inhibited OE33 cell growth in single dose MTT assays (EC50= 10 uM) and, more potently, in multi-dose colony formation assays (EC50=1.3 uM)NADI-351 is 15 times more potent than IMR-1 in an NTC AlphaScreen assay.NADI-351 selectively disrupted Notch1 transcription complexes, inhibited recruitment of Notch1 to the NTC (Notch Ternary Complex) and to the HES1 promoter, and reduced Notch1 recruitment to target genes.NADI-351 inhibits tumor growth in Notch-dependent cancers and does not exert gastrointestinal toxicity associated with goblet cell metaplasia.NADI-351 selectively inhibits stem-like esophageal adenocarcinoma (EAC) cell populations.

III-31-C is a (hydroxyethyl)urea γ-secretase inhibitor. III-31-C inhibits Aऔ production with an IC50 of 10 nM in the cell-free γ-secretase assay and 200 nM in APP-transfected cells. III-31-C can be used in Alzheimer's disease research.

(9R)-RO7185876 (Compound example 16) is a γ-secretase inhibitor. (9R)-RO7185876 inhibits Αβ42 secretion. (9R)-RO7185876 can be used for the researches of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, multi-infarct dementia, dementia pugilistica or Down syndrome.

NCB-0970 is the negative control of NCB-0846. (R)-Norfluoxetine is a potent serotonin re-uptake inhibitor, with a Ki of 13 nM. (R)-Norfluoxetine can be used for the research of depression.

EXQ-2d is the inhibitor for tankyrase and inhibits TNKS1 and TNKS2 with an IC50 of 48.8 nM and 13.8 nM (pIC50=7.31 and 7.86). EXQ-2d inhibits WNT/β-catenin signaling pathway with IC50 of 515 nM. EXQ-2d exhibits anti-proliferative activity in cancer cells COLO 320DM and RKO with GI50 of 4.9 μM and 77 μM.

BMD4503-1 is a quinoxaline derivative. BMD4503-1 can inhibit the LRP5/6-Sclerostin interaction and regulate the Wnt signaling pathway.

21H7 is a selective inhibitor of the Wnt/b-catenin pathway. 21H7 markedly inhibits the growth of HFs. 21H7 potently decreases growth of breast and colon cancer cells.

1(R),2(S)-epoxy Cannabidiol (Compound 2a) is a structural analogue of phytocannabinoidsphytocannabinoids. 1(R),2(S)-epoxy Cannabidiol exhibits potent inhibitory activity against Wnt/β-catenin pathway. 1(R),2(S)-epoxy Cannabidiol is promising for research of neuroprotective agents.

GSK-3β probe-1 (10c) is a GSK-3β probe (Ex = 341 nm, Em= 574nm, ɛ= 3.51 × 104L/mol·cm−1) and can be be used in the study of Alzheimer's disease.

2-Cyanoethylalsterpaullone (compound 7) is an Alsterpaullone derivative and a PI3K/Akt signalling activator which promotes epithelium repair. Hydroxy celecoxib can be utilized in asthma research.

WAY-606344 (Compound 97) is a Casein kinase 1δ inhibitor. WAY-606344 is promising for research of Alzheimer's disease.

CK1δ/CK1ε liagnd-1 is the ligand for CK1δ/CK1ε that can be used for synthesis of CK1 PROTAC degrader AH078.

AH078 (compound 37) is a PROTAC degrader that selectively targets CK1δ and CK1ε, and has low targeting for CK1α.

(R,R)-BMS-986397 is a CK1α degrader (DC50 between 0.1-0.5 pM). (R,R)-BMS-986397 can be used in anti-leukemia research.

GLPG-1690 is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.

TWS119 is a GSK-3β inhibitor with IC50 of 30 nM.

BMS-708163 is a potent, selective γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, respectively.

​​Toxoflavin (Xanthothricin)​​ is a dual-function bioactive compound with multimodal therapeutic potential.

CKIα inhibitor A86 is a groundbreaking pan-specific inhibitor targeting Casein Kinase I (CSNK1), with a remarkable binding affinity (Kd=1-10 nM) and a specific Kd of 9.8 nM for CKIα. Beyond its primary activity, this compound also demonstrates dual inhibitory effects on the transcriptional kinases CDK7 and CDK9. Notably, it exhibits minimal to no inhibition against CDK8, CDK13, CDK11a, CDK11b, and CDK19, highlighting its selective pharmacological profile.

FL-1607, a novel Fam20C inhibitor, has shown remarkable anti-proliferative effects in triple-negative breast cancer (TNBC) cells. This compound induces apoptosis and significantly reduces the migration ability of MDA-MB-468 cells, underscoring its potential as a promising therapeutic agent for TNBC treatment.

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.

CHIR-99021 HCl is a potent and selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β), a key enzyme involved in regulating various cellular processes, including metabolism, cell proliferation, and differentiation. By inhibiting GSK-3β, CHIR-99021 HCl modulates downstream signaling pathways, particularly the Wnt/β-catenin pathway, leading to significant biological effects both in vitro and in vivo.

I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM) and is inactive for other H2S/sulfane sulfur-producing enzymes.?I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST.

PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification

A potent, highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 4 nM for CK1δ.

E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.E722-2648 (Compound C-1) inhibited β-catenin/BCL9 complexes at concentrations as low as 1 uM in BCL9-dependent CRC cell lines, Colo320 and HCT116.E722-2648 (Compound C-1) inhibited the expression of bona fide downstream Wnt/β-catenin target genes, AXIN2 and CD44, in the β-catenin/BCL9-dependent CRC cell lines.E722-2648 (Compound C-1) disrupted cholesterol homeostasis via increased cholesterol esterification and lipid droplet accumulation.E722-2648 (Compound C-1) demonstrated antitumorigenic activity in CRC cell lines and xenograft mouse models.

Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).

Rhonin is a first small-molecule ligand of the RHO GDP-dissociation inhibitor 1 (RHOGDI1), binds to RHOGDI (Ki=2.2 uM), is an inhibitor of Hh-induced osteogenesis.Rhonin interferes with its function by disrupting the interaction between RHOGDI and RHO GTPases.Rhonin alters the subcellular localization of RHO GTPases.Rhonin inhibited RHOGDI1-mediated extraction of RAC1 from liposomes, Rhonin increased the levels of GTP-bound RHO GTPases, did not alter the total levels of the three RHO GTPasesRhonin an inhibitor of Hh-induced osteogenesis, but does not efficiently target canonical Hh signaling and SMO, directly targets RHOGDI, impairs RHOGDI function.

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.

LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.