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GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models.

Combretastatin A4 (CA4) is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM).

Fosbretabulin Disodium (CA 4P), a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium(Combretastatin A4 disodium phosphate) inhibits the polymerization of tubulin (IC50: 2.4 μM), and also disrupts tumor vasculature.

Bretisilocin is an agonist of the 5-HT2A receptor and exhibits antidepressant activity.

Fosbretabulin is a natural cis-stilbene that interferes with cellular tubulin dynamics and selectively destroys tumor blood vessels.

Combretastatin A-1 is a potent microtubule inhibitor with anti-tumour and anti-vascular activity, acting through microtubule protein depolymerisation-mediated inactivation of AKT to inhibit the Wnt/β-catenin pathway, and can be used to study hepatocellular carcinoma.

Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a tubulin-binding microtubule polymerization inhibitor targeting the colchicine-binding site. By inducing tubulin depolymerization, it inhibits the Wnt β-catenin pathway and deactivates AKT, possessing both anti-tumor and anti-vascular properties.

[(2-Di-tert-butylphosphino-3,6-dimethoxy-2',4',6'-triisopropyl-1,1'-biphenyl)-2-(2'-amino-1,1'-biphenyl)]palladium(II) methanesulfonate is a useful organic compound for research related to life sciences. The catalog number is T64584 and the CAS number is 1536473-72-9.

(tBuBrettPhos Pd(allyl))TfOH salt is a useful organic compound for research related to life sciences and the catalog number is T64621.

BrettPhos Pd G4 is a useful organic compound for research related to life sciences. The catalog number is T64764 and the CAS number is 1599466-83-7.

AdBrettPhos Pd G3 is a useful organic compound for research related to life sciences and the catalog number is T67255.

Combretastatin A1 phosphate, a potent vascular disruptive agent, exhibits anti-angiogenic effects on tumors and holds potential for research on pancreatic neuroendocrine tumors.

Bretylium tosylate is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters, a available antiarrhythmic drug for ventricular arrhythmias.

Combretol has leishmanicidal activity, it showed moderate activity (growth inhibition 87.3 and 73.0 %, respectively, at 50 μM) against a multidrug-resistant L. tropica line. Combretol also shows weakly active cytotoxic activity.

Montbretin A, an acylated flavonol glycoside found in C. crocosmiiflora, exhibits antidiabetic activity.

Laminin β2 (Engelbreth-Holm-Swarm murine sarcoma basement membrane) is a crucial structural component in animal tissues, forming part of the framework that supports tissue architecture. It interacts with type IV collagen through entactin and basement membrane proteoglycans and associates with cell membranes via integrin receptors, dystroglycan complexes, and Lutheran blood group glycoproteins. Additionally, it contains functional domains that facilitate collagen binding, cell adhesion, heparin interactions, and promote neurite outgrowth.

L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist and benzolactam derivative, known for reversing glucocorticoid-induced inhibition of GH secretion. L-692429 exhibits high affinity for the G protein-coupled receptor and is useful in studying acromegaly and obesity.

HDAC-IN-4, a selective HDAC6 and HDAC10 inhibitor (pIC50s: 7.2 and 6.8 in the BRET assay), exhibits antitumoral activity.

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

Potent inhibitor of CDK16 and CDK14 (IC50 values are 6 and 140 nM, respectively in kinase activity assay; IC50 = 563 nM for CDK14 in BRET assay). Also binds CDK2 (IC50 = 493 nM). Inhibition reversible upon compound wash-out. Control for FMF-04-159-2 (Cat. No. 7158).

CBP-IN-1 (compound 12) is a potent CBP inhibitor with an IC50 of 1.5 nM, additionally suppressing CBP BRET and BRD4(1) with IC50 values of 690 nM and 3100 nM, respectively [1].

Tianeptine metabolite MC5, an active derivative of the atypical antidepressant tianeptine produced through β-oxidation, exhibits selective G protein activation in bioluminescence resonance energy transfer (BRET) assays. Utilizing HEK293T cells expressing the human μ-opioid receptor (MOR) over the human δ-opioid receptor (DOR; EC50s = 0.454 and >100 µM, respectively), it demonstrates specificity. Moreover, this metabolite reduces immobility in wild-type mice during the forced swim test at a dose of 30 mg/kg, an effect not observed in MOR knockout mice, suggesting its antidepressant-like activity is MOR-dependent.

JHU37160 (JHU 37160) is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

JHU37152 (JHU 37152) is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.