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HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. -
RAR agonist
Tretinoin is an endogenous agonist for retinoic acid receptors with IC50 value of 14 nM for RAR-alpha, RAR-beta and RAR-gamma receptors). -
SMO Antagonist
LY2940680 has been shown to affect a cancer cell signaling pathway initiated by the Hedgehog (Hh) protein. -
GSK-3 inhibitor
CHIR-98014 is a very potent, selective, cell-permeable reversible inhibitor of GSK-3. -
p38 MAPK inhibitor
SB 203580 hydrochloride (Adezmapimod hydrochloride) (RWJ 64809 hydrochloride) is a widely used p38 MAPK inhibitor.
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pan-Notch inhibitor
BMS-983970 is an oral pan-Notch inhibitor for the treatment of multiplecancers. -
Notch inhibitor
Notch inhibitor 1 is a potent Notch inhibitor, with IC50s of 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively. Used in the research of cancer. -
pan-Akt inhibitor
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5/18/8 nM, 620-fold selectivity over PKA. -
PDE7/GSK3 inhibitor
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. -
BMP type I receptor inhibitor
LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50??500 nM). -
CK1 inhibitor
Epiblastin A is an inhibitor of Casein Kinase 1 (CK1) that engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs). -
GSK-3 inhibitor
GSK3 Inhibitor XIII (GSK3i XIII) is an ATP-binding site inhibitor of GSK-3. -
Notch Inhibitor
CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity. -
ATP-competitive CK2 inhibitor
Ellagic acid hydrate is a natural antioxidant, and acts as a potent and ATP-competitive CK2 inhibitor, with an IC50 of 40 nM and a Ki of 20 nM. -
BMP signaling inhibitor
LDN193189 HCl (DM-3189) is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β. -
natural product
L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway. - Casein Kinase 2 Substrate Peptide is a common CK2 substrate peptide. Casein Kinase 2 Substrate Peptide is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). Casein Kinase 2 Substrate Peptide can be used for protein kinase CK2 activity determination.
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YAP-TEAD Inhibitor
IAG933 is a potent YAP-TEAD inhibitor that targets the YAP/TAZ-TEAD interaction, demonstrating significant anti-tumor effects by promoting apoptosis in cancer cells. With an IC50 value of 9 nM against Avi-human TEAD4217-434, IAG933 serves as a valuable tool for studies investigating the YAP signaling pathway and its role in oncogenesis. Its oral bioavailability further enhances its utility in in vivo research applications focused on cancer therapeutics. -
YAP/TAZ Inhibitor
VT3989 is a potent YAP/TAZ inhibitor, targeting the essential Hippo signaling pathway regulators. It demonstrates significant inhibitory activity against firefly luciferase, with an IC50 value of less than 0.1 μM. This compound is ideal for research applications focused on understanding the roles of YAP/TAZ in cancer biology and cellular signaling pathways. -
pan-TEAD Inhibitor
GNE-7883 is a pan-TEAD inhibitor that disrupts the interaction between YAP/TAZ and TEAD transcription factors. This compound reduces chromatin accessibility at TEAD-binding sites and inhibits cell proliferation across various cell line models, demonstrating significant anti-tumor effects in vivo. Additionally, GNE-7883 addresses both intrinsic and acquired resistance to KRAS G12C inhibitors in multiple preclinical settings by targeting YAP/TAZ activation, making it a valuable tool for cancer research. -
Wnt/β-Catenin Inhibitor
MSAB is a potent and selective Wnt/β-catenin signaling inhibitor. By binding to β-catenin, it promotes its degradation and effectively downregulates Wnt/β-catenin target genes. MSAB demonstrates significant anti-tumor activity, particularly in Wnt-dependent cancer cell lines, making it a valuable tool for cancer research and therapeutic development targeting aberrant Wnt signaling. -
Natural Retinoid
9-cis-Retinal is a natural retinoid that serves as a crucial signaling molecule in visual processes. It is produced from dietary 9-cis-β-carotene through enzymatic cleavage. This compound exhibits high-affinity binding to cellular retinol-binding proteins CRBP-I and CRBP-II, with dissociation constants of 8 nM and 5 nM, respectively. 9-cis-Retinal plays a significant role in promoting differentiation and maturation of rod photoreceptors in retinal organoid models, making it valuable for research in vision science and photoreceptor development. -
Smo Agonist
GSA-10 is a potent agonist of the smooth (Smo) receptor, playing a crucial role in mediating Hedgehog (Hh) signaling pathways. This compound exhibits significant osteogenic activity and is valuable in regenerative medicine and research on cancer pathologies. Additionally, GSA-10 can be utilized in studies focused on adipogenesis and fat development, making it a versatile tool in biological research. -
Dishevelled Protein PDZ Domain Inhibitor
3289-8625 is a potent inhibitor of the PDZ domain of Dishevelled (Dvl) protein, exhibiting a Kd of 10.6 μM. This compound effectively inhibits Wnt signaling pathways and demonstrates a significant impact on prostate cancer PC-3 cell growth, with an IC50 of 12.5 μM. 3289-8625 is valuable for research involving embryonic development and cancer biology. -
Neurogenesis Inducer
Neurodazine is a neurogenesis inducer that promotes the differentiation of pluripotent cells into neuronal lineages. This compound activates the Wnt and Shh signaling pathways, facilitating neural development and potentially improving neuroregeneration applications. Neurodazine is suitable for research in developmental biology, neuroscience, and regenerative medicine. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
RAR Agonist
EC23 is a retinoid analogue that acts as a retinoic acid receptor (RAR) agonist. This compound prompts neuronal differentiation, making it a valuable tool for studying neurodevelopmental processes and related disorders. Its stability enhances its suitability for various biological assays and research applications in the field of neurobiology. -
CDK Inhibitor
NSC693868 is a selective inhibitor of cyclin-dependent kinases CDK1 and CDK5, demonstrating IC50 values of 600 nM and 400 nM, respectively. This compound also exhibits weaker inhibition of GSK3β with an IC50 of 1 µM and does not affect CDC25 activity. NSC693868 is employed in research to elucidate the functions of CDK1 and CDK5 within various cellular signaling pathways. -
DKK1 Inhibitor
Gallocyanine chloride is a DKK1 inhibitor that targets the DKK1/LRP6 interaction, exhibiting an IC50 of 6.38 μM. This compound is relevant for research into Alzheimer's disease and related neurodegenerative tauopathies, as it activates the Wnt signaling pathway and promotes β-catenin accumulation. Additionally, Gallocyanine chloride demonstrates anti-metastatic, anti-inflammatory, and anti-fibrotic properties, and can serve as a fluorescent probe for the detection of superoxide anion radicals. -
GSK-3α/β Inhibitor
(E/Z)-BIO-acetoxime is a potent and selective inhibitor of GSK-3α/β, exhibiting an IC50 of 10 nM. This compound demonstrates exceptional selectivity with over 200-fold preference against CDK5/p25, CDK2/cyclin A, and CDK1/cyclin B, with IC50 values of 2.4, 4.3, and 63 μM, respectively. Its strong inhibitory activity makes it a valuable tool for research focused on signaling pathways involved in cell proliferation, differentiation, and apoptosis. -
SIRT Inhibitor
Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity. -
NLRP3 Activator
Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin is a NLRP3 activator. Nigericin shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin induces pyroptosis through caspase 1/GSDMD in TNBC. -
δ-Secretase Inhibitor
δ-Secretase inhibitor 11 is a potent and selective inhibitor targeting δ-secretase, displaying an IC50 of 0.7 μM. This compound effectively interacts with both the active and allosteric sites of δ-secretase, resulting in the attenuation of tau and amyloid precursor protein cleavage. Its oral bioavailability and blood-brain barrier penetration make it suitable for in vivo studies, particularly in transgenic mouse models. δ-Secretase inhibitor 11 is a valuable tool for Alzheimer's disease research, facilitating investigations into the mechanisms underlying synaptic dysfunction and cognitive impairments. -
CK2 Inhibitor
CK2-TN03 is an ATP-competitive inhibitor of casein kinase 2 (CK2), demonstrating an IC50 of 165 nM and a Ki of 20 nM. This compound effectively inhibits CK2-mediated activation of survivin and reduces phosphorylation levels of critical proteins such as BRD4/MYCN and AKT1. CK2-TN03 has shown significant anti-neuroblastoma effects by promoting mitotic catastrophe and apoptosis in cancer cells, making it a valuable tool for research focused on neuroblastoma. -
p53 Activator/Wnt Inhibitor
PAWI-2 is a p53 activator and Wnt inhibitor that targets β3-KRAS signaling independently of KRAS. This compound selectively inhibits the phosphorylation of TBK1, resulting in the activation of apoptotic pathways, evidenced by increased caspase-3/7 activity and PARP cleavage. Additionally, PAWI-2 facilitates the translocation of optineurin into the nucleus and induces G2/M cell cycle arrest. It effectively reverses cancer stemness and overcomes drug resistance in integrin β3 KRAS-dependent human pancreatic cancer stem cells, demonstrating significant tumor growth inhibition in orthotopic xenograft mouse models. -
YAP activator
PY-60 is a potent and selective small-molecule activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a dissociation constant (Kᴅ) of 1.4 µM. By directly binding to ANXA2, PY-60 antagonizes its inhibitory regulation of YAP, thereby enhancing YAP-dependent gene expression and promoting transcriptional activation within the Hippo signaling pathway. -
actin polymerization inhibitor
Cytochalasin D (also known as Zygosporin A) is a cell-permeable fungal metabolite and a potent inhibitor of actin polymerization. It binds to G-actin, thereby disrupting the G-actin–cofilin interaction and preventing cofilin association with F-actin. Through this mechanism, Cytochalasin D reduces both actin polymerization and depolymerization rates in living cells, leading to profound effects on cytoskeletal organization and cell morphology. In addition, Cytochalasin D suppresses exosome release, consequently decreasing survivin levels within the tumor microenvironment. It also promotes phosphorylation and cytoplasmic retention of YAP, implicating it in the regulation of mechanotransduction and tumor cell signaling. -
Wnt inhibitor
Cardionogen 1 (CDNG1/vuc230) is an inhibitor of the Wnt signaling pathway that suppresses Myc-induced liver tumorigenesis. In zebrafish embryos, Cardionogen 1 inhibits cardiomyocyte formation when administered before gastrulation, but promotes cardiomyocyte formation when applied during or after gastrulation. It holds potential for research in cancer and cardiovascular disease. -
BRD4/CK2 inhibitor
BRD4/CK2-IN-1 is the first highly potent and orally active dual inhibitor of BRD4 and casein kinase 2 (CK2), with IC₅₀ values of 180 nM and 230 nM, respectively. It exhibits strong anticancer activity with minimal toxicity, and induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC) cells.

