Stem Cell and Derivatives

GKI-1 HCl is a Greatwall (GWL) kinase inhibitor that inhibits hGWLFL and hGWL-KinDom.The inhibitory effect of GKI-1 HCl on ROCK1 is more significant.

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2).

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Dog sCD14. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Dog sCD14. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Dog sCD14, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Dog sCD14 in the samples is then determined by comparing the OD of the samples to the standard curve.

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.

IHR-1, a Smo inhibitor (IC50 7.6 nM), blocks Hedgehog pathway, not Wnt/Notch, and prevents Smo in primary cilium.

PROTAC YAP degrader-1, a targeted proteolysis promoting chimeric molecule, both degrades the YAP protein and inhibits its nuclear localization. This compound is formulated with Demethyl-NSC682769 as the target protein ligand, and utilizes (R,S,R)-AHPC-PEG2-C2-boc, which is the E3 ubiquitin ligase ligand + Linker conjugate. The linker incorporated in the design is Acid-PEG2-C2-Boc.

FH535, a Wnt/β-catenin signaling and PPAR inhibitor, exhibits anti-tumor activities.

BI-1408 is a modulator potent of γ secretase (IC50: 0.04 μM for Aβ42).

JAK-IN-30 (compound 31) is a water-soluble inhibitor of Janus kinases (JAKs), demonstrating inhibitory potency with half-maximal inhibitory concentration (IC50

CID-5056270 has anticancer activity and can inhibit lung cancer, anal cancer, bladder cancer, cervical cancer, vulvar cancer, penile cancer, Burkitt's lymphoma

GS-829845 is a JAK1 inhibitor, the main component of the active metabolite of Filgotinib, which is approximately 10-fold less potent and has a longer half-life

Brepocitinib P-Tosylate (PF-06700841 P-Tosylate) is a potent dual inhibitor of Janus kinase 1 (JAK1) and TYK2 (IC50s of 17 nM and 23 nM, respectively).

HPI 1 suppresses Hh pathway: IC50 = 1.5 μM (Shh, SAG), 4 μM (Gli2), 6 μM (Gli1) in Shh-LIGHT2 cells.

JAK-IN-25 (compound 19), a potent JAK inhibitor, exhibits IC50 values of 6 nM for TYK2, 21 nM for JAK1, 8 nM for JAK2, and 1051 nM for JAK3.

FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2)

Cyanoacetohydrazide (Cyanoacetic hydrazide) is an anti-TB drug. It has also been used to derive compounds that may have antitumor properties.

Porcn-IN-1 (Porcupine-IN-1) is an effective porcupine inhibitor (IC50: 0.5±0.2 nM).

Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex. Toxoflavin also acts as an inhibitor of KDM4A.

STAT3-IN-39 (compound 10K) is an orally active inhibitor of STAT3, demonstrating effective inhibition of STAT3 phosphorylation with an IC50 of 0.47 μM in NIH-3T3 cells. It hinders TGF-β1-induced fibrotic responses and prevents epithelial-mesenchymal transition in A549 cells. STAT3-IN-39 is applicable for research related to idiopathic pulmonary fibrosis.

TNIK-IN-2 is an inhibitor Traf2- and Nck-interacting protein kinase (TNIK, IC50 = 1.33 μM)) which is a downstream signal protein of the Wnt/β-catenin pathway.