bcat

BCAT-IN-2 is an orally active and selective inhibitor of mitochondrial branched-chain aminotransferase (BCATm), inhibits BCATm and BCATc, and is used in obesity and dyslipidemia.

BCAT-IN-1 is an orally active and selective BCATm inhibitor and a potential BCAT2 modulator, used in studies of metabolic diseases.

BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective e

BAY-069 is an inhibitor. BAY-069 inhibited branched-chain amino acid transaminase 1 (BCAT1) at IC50:31 nM and branched-chain amino acid transaminase 2 (BCAT2) at IC50:153 nM. BAY-069 is a novel (trifluoromethyl) pyrimidine dione chemical probe, which can be used for anticancer research.

BCAT-IN-4 is a potent BCAT inhibitor with an IC50 value of 2.35 μM for hBCATc. BCAT-IN-4 has anticancer activity and can be used to study pancreatic ductal adenocarcinoma.

Bobcat339 is a novel cytosine-based TET enzyme inhibitor (IC50s: 33/73 uM for TET1/2), but not DNMT3a, does not inhibit the DNA methyltransferase DNMT3a.

Bobcat339 hydrochloride is a selective 10 11 translocation (TET) dioxygenase inhibitor that inhibits TET1 and TET2.Bobcat339 hydrochloride induces TET3 protein degradation and also stimulates the expression of AGRP, NPY, and VGAT in a TET3-dependent manner in mouse and human neuronal cells. VGAT expression, which can be used to study transient anorexia nervosa.

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

IWP-2 is a Wnt pathway inhibitor (IC50=27 nM) and an ATP-competitive CK1δ inhibitor (IC50=40 nM for M82FCK1δ). IWP-2 inhibits self-renewal of embryonic stem cells and has been used in stem cell and organoid research.

BML-284 (Wnt agonist 1) is a potent, selective and , cell-permeable Wnt signaling activator.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Adavivint (SM04690) is a selective inhibitor of the typical Wnt signaling pathway. In SW480 cells, EC50=19.5 nM was measured using high-throughput TCF/LEF reporter gene experiments.

SKL2001, an agonist of the Wnt/β-catenin pathway, can disrupt the Axin/β-catenin interaction.

MSAB is a selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes.

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

Wnt pathway activator 2, with an IC50 of 13 nM, is a potent Wnt activator.

DK419 is an orally active inhibitor of Wnt/β-catenin signaling, with an IC50 of 0.19 μM. DK419 decreases protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin.It also induces production of pAMPK.

CCT 031374 hydrobromide is a TCF/β-catenin inhibitor with antitumor activities.

FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2) by binding to an allosteric site on intracellular loop 3 (ICL3) of FZD4. This interaction changes the receptor's conformation and inhibits the WNT/β-catenin signaling pathway.

Gossypolone is is a proposed major metabolite of gossypol. Gossypolone reduces Notch/Wnt signaling and induces apoptosis.

GSK-3β inhibitor 8 (GSK3β Inhibitor XVIII) is a potent and selective GSK-3β inhibitor with an IC50 value of 64 nM.GSK-3β inhibitor 8 is a thienopyrimidine derivative that negatively regulates the Wnt signaling pathway and stimulates β-cell proliferation.

Carboxylesterase-IN-3 is a potent inhibitor of Carboxylesterase Notum (IC50 ≤ 10 nM).Carboxylesterase-IN-3 has the potential to study cancer diseases.

NRX-103094 is a potent enhancer of the interaction between β-catenin and the homologous E3 ligase SCFβ-TrCP, increasing the affinity of pSer33/Ser37 β-catenin for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM.

NRX-252114 (NRX252114) induces degradation of mutant β-catenin NRX-252114 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP, and is able to enhance the binding of pSer33/S37A β-catenin to β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. Kd is 0.4 nM.