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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
TET2 inhibitor
TFMB-(S)-2-HG is a potent inhibitor of TET2 and EglN prolyl hydroxylases. It downregulates Wnt3a and intranuclear β-catenin protein expression, and inhibits osteogenic differentiation of cells. TFMB-(S)-2-HG shows potential for research in acute myeloid leukemia (AML). -
Wnt inhibitor
Zamaporvint (RXC004) is an orally active and selective Wnt pathway inhibitor that targets the membrane-bound O-acyltransferase Porcupine. By inhibiting Wnt ligand palmitoylation, it blocks Wnt ligand secretion and downstream pathway activation. Zamaporvint exhibits a favorable pharmacokinetic profile and shows potent antiproliferative activity in Wnt ligand-dependent colorectal and pancreatic cancer cell lines. With multiple antitumor mechanisms, it is a promising agent for cancer research. -
CK2/ERK8 inhibitor
TMCB (CK2/ERK8-IN-1) is a dual inhibitor of casein kinase 2 (CK2) and ERK8 (MAPK15/ERK7), with a Ki of 0.25 µM for CK2 and IC50 values of 0.50 µM for both targets. It also exhibits binding affinity for PIM1 (Ki = 8.65 µM), HIPK2 (Ki = 15.25 µM), and DYRK1A (Ki = 11.9 µM). CK2/ERK8-IN-1 demonstrates pro-apoptotic activity and is a useful tool for studying kinase-mediated cell survival pathways. -
TAK1 inhibitor
HS-276 is an orally bioavailable, potent, and highly selective inhibitor of transforming growth factor-β–activated kinase 1 (TAK1), with a Kᵢ of 2.5 nM. It exhibits strong inhibition of TAK1 and moderate activity against a panel of other kinases, including CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with respective IC₅₀ values ranging from 8.25 to 5585 nM. HS-276 is a valuable tool for investigating TAK1-mediated signaling pathways and holds therapeutic potential for inflammatory conditions such as rheumatoid arthritis (RA). -
Casein Kinase inhibitor
BTX-A51 (Casein Kinase Inhibitor A51) is a potent, orally bioavailable inhibitor of casein kinase 1α (CK1α). It effectively induces apoptosis in leukemia cells and demonstrates strong anti-leukemic activity in preclinical models, making it a promising therapeutic candidate for hematologic malignancies. -
Wnt/β-catenin Inhibitor
CCT036477 is a selective inhibitor of the Wnt/β-catenin signaling pathway that effectively disrupts β-catenin-mediated transcription without affecting its overall levels. This compound demonstrates significant anti-proliferative effects on various cancer cell lines and impairs embryonic development. Additionally, CCT036477 downregulates the expression of key Wnt target genes, including PPARδ, Cyclin D1, TCF4, and ID2, making it a valuable tool for research in cancer biology and developmental studies. -
Akt Inhibitor
Ipatasertib tosylate is a potent and selective ATP-competitive inhibitor of pan-Akt, exhibiting IC50 values of 5, 18, and 8 nM for Akt1, Akt2, and Akt3, respectively. By inhibiting Akt, Ipatasertib tosylate activates FoxO3a and NF-κB, resulting in p53-independent activation of PUMA and subsequent apoptosis in cancer cells. This compound demonstrates significant anti-tumor activity in xenograft mouse models, making it a valuable tool for cancer research and therapeutic development. -
Allosteric Akt Inhibitor
MK-2206 free base is a highly potent and selective allosteric inhibitor of the Akt signaling pathway, exhibiting IC50 values of 8 nM, 12 nM, and 65 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anticancer properties, particularly against breast cancer cell lines, as well as those harboring PIK3CA mutations and PTEN loss. MK-2206 free base is valuable for research applications focused on cancer biology and therapeutic development targeting the Akt pathway. -
Allosteric Akt Inhibitor
MK-2206 is a highly potent and selective allosteric inhibitor of the Akt signaling pathway, exhibiting IC50 values of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anticancer activity, particularly in breast cancer cell lines and those harboring PIK3CA mutations or loss of PTEN function. MK-2206 is valuable for research investigating Akt's role in cancer progression and therapeutic resistance. -
Casein Kinase Inhibitor
Hematein is an allosteric inhibitor of casein kinase II, exhibiting an IC50 of 0.74 μM. It demonstrates significant biological activity by inhibiting Akt/PKB Ser129 phosphorylation and the Wnt/TCF signaling pathway. Research applications include studying apoptosis in lung cancer cells, making it a valuable reagent for cancer biology investigations. -
Wnt/β-catenin/NF-κB/AP-1 Inhibitor
Chikusetsusaponin IVa methyl ester is a natural triterpenoid saponin that functions as a Wnt/β-catenin, NF-κB, and AP-1 inhibitor. It induces G0/G1 cell cycle arrest and apoptosis in colon cancer cells through the inhibition of the Wnt/β-catenin signaling pathway. Additionally, this compound significantly decreases the production of nitric oxide, prostaglandin E₂, and pro-inflammatory cytokines, while downregulating iNOS and COX-2 levels. Chikusetsusaponin IVa methyl ester is valuable for research focused on colorectal cancer and inflammatory processes. -
HDAC/CK2 Inhibitor
HDAC/CK2-IN-1 is an inhibitor targeting histone deacetylases HDAC1 and HDAC6, with IC50 values of 1.46 μM and 0.66 μM, respectively, as well as casein kinase 2 (CK2) with an IC50 of 3.67 μM. This compound demonstrates significant antiproliferative effects on various cancer cell lines, including Jurkat, MCF-7, HCT-116, and HL-60. It serves as an important research tool for studying the roles of histone modifications and CK2 in tumor biology and could have potential implications in the development of cancer therapeutics. -
CK2/HDAC Inhibitor
IOR-160 is a dual inhibitor targeting casein kinase 2 (CK2) and histone deacetylases (HDACs). It showcases high selectivity for CK2, with an IC50 of 1.7 nM, and demonstrates broad inhibitory effects on HDACs 1, 2, 3, and 6, with IC50 values of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively. Through the inhibition of AKT phosphorylation and the enhancement of acetylated α-tubulin levels, IOR-160 effectively modulates critical cellular signaling pathways. This compound is particularly relevant in research focused on triple-negative breast cancer, where it has been shown to inhibit tumor growth and reduce tumor burden. -
HDACs Inhibitor
NL-103 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 21.3 nM, 57 nM, 74 nM, and 680 nM for HDAC1, HDAC2, HDAC3, and HDAC6, respectively. This compound also targets the Hedgehog signaling pathway, leading to the downregulation of Gli2 expression. NL-103 is primarily utilized in cancer research, providing valuable insights into HDAC regulation and its role in tumor biology. -
HDAC6 Inhibitor
(S)-Trichostatin A is a selective inhibitor of HDAC6, demonstrating IC50 values of 9.88 nM and 11.1 nM for Zebrafish and Human HDAC6, respectively. It exhibits weak inhibition of other human HDACs, making it a valuable tool for studying HDAC6's role in cellular processes. This compound is useful in research applications related to cancer, neurodegenerative diseases, and epigenetic regulation. -
Wnt/β-catenin Inhibitor
Windorphen is a selective Wnt/β-catenin signaling inhibitor that specifically interferes with the c-terminal transactivation domain of β-catenin-1, while leaving β-catenin-2 unaffected. This compound targets p300, effectively disrupting the interaction between β-catenin and p300 without impacting CBP. Windorphen is valuable for research applications focused on β-catenin-related pathways, cancer biology, and developmental processes. -
GSK-3β/G9a Inhibitor
GSK-3β/G9a-IN-1 is a selective inhibitor of GSK-3β and G9a, acting through competitive mechanisms with IC50 values of 0.8 μM and 1.1 μM, respectively. This compound is effective in lowering tau phosphorylation and reducing Aβ aggregation, making it relevant for Alzheimer's disease research. Additionally, GSK-3β/G9a-IN-1 influences chromatin dynamics by inhibiting H3K9me2 and modulating members of the SAGA complex. Its ability to improve memory and restore social behaviors highlights its potential as a therapeutic agent in neurodegenerative conditions. -
Akt Inhibitor
GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays -
γ-secretase inhibitor
Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. -
γ-secretase inhibitor
PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM . -
γ-Secretase Inhibitor
BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease. -
Casein kinase inhibitor
Potent and selective casein kinase 1ε (CK1ε) and CK1δ inhibitor (IC50 values are 7.7 and 14 nM respectively) that displays > 30-fold selectivity over 42 other common kinases. Inhibits PER protein nuclear translocation (EC50 = 290 nM) causing phase shifts in circadian rhythms and attenuates methamphetamine-stimulated locomotion in vivo. -
Notch inhibitor
LY3039478 is a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested. -
PKA, PKG, Casein Kinase I and II inhibitor
A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM). -
gamma-secretase inhibitor
Flurbiprofen Axetil is potentnon-steroidal anti-inflammatory drug(NSAID). -
sFRP-1 inhibitor
WAY-316606 is a small molecule inhibitors of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. -
CK2 inhibitor
TTP 22 is a high affinity, casein kinase 2 (CK2) inhibitor (IC50= 0.1uM, Ki= 40nM). In addition, TTP 22 shows selectivity for CK2 over JNK3, ROCK1, and MET (inhibitory effects displayed at greater than 10 uM). TTP 22 is highly conserved serine/threonine protein kinase that is also involved in cell proliferation, cell differentiation and apoptosis. -
GSK-3β inhibitor
1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25. -
Potent porcupine inhibitor
Porcn-IN-1 is potent porcupine inhibitor with an IC50 of 0.5??0.2 nM.
