non-selective

PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 µM)

Tetraethylammonium chloride is a quaternary ammonium compound. It is a non-selective potassium channel blocker. It is a good substrate for organic cation transporter proteins and has antitumor properties.

Bupranolol is an antagonist of β2-adrenergic receptor and has been used for angina pectoris, hypertension, glaucoma, cardiac arrhythmia and as an antithrombotic.

TRPM4-IN-1 (4-chloro-2-(2-(2-chlorophenoxy)acetamido)benzoic acid) is a potent and selective inhibitor of TRPM4 with an IC50 of 1.5 μM.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

Resmetirom (MGL-3196) is a THR-β agonist (EC50=0.21 μM), with high selectivity and oral activity. Resmetirom can be used in the research of non-cirrhotic and non-alcoholic steatohepatitis.

GW4869 (GW69A) is a selective and non-competitive inhibitor of neutral sphingomyelinase N-SMase (IC50=1 μM). GW4869 also inhibits exosome synthesis/release and is commonly used in exosome-related studies.Usually prepared as a suspension for experiments.

Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity. Mirdametinib exhibits antitumor activity by inhibiting p-ERK1/2 expression and inducing apoptosis.

Selvigaltin (GB1211) is an orally administered, highly selective small-molecule inhibitor of galectin-3 (Gal-3) with an IC₅₀ value of 12 nM in rabbits, exhibiting anticancer and anti-fibrotic activity. Selvigaltin reduces galectin-3 levels in the liver and decreases biomarkers of inflammation (cellular foci) and fibrosis (PSR, SHG), while simultaneously lowering the mRNA and protein expression of inflammatory and fibrotic biomarkers (IL-6, TGF-β3, SNAI2, collagen). Selvigaltin also restores T-cell activity and reduces tumor growth and metastasis. Selvigaltin is suitable for use in studies of liver fibrosis, non-alcoholic steatohepatitis (NASH), and tumors.

Omaveloxolone (RTA-408) is an oral, potent, and selective activator of the nuclear factor erythropoietin-related factor 2 (Nrf2) pathway, as well as a low-potency PPARγ agonist. Omaveloxolone inhibits osteoclast formation by suppressing the STING-dependent NF-κB signaling pathway. Omaveloxolone is being investigated for use in ALS, multiple sclerosis, non-alcoholic steatohepatitis, neurodegenerative diseases, and oncology research.

ART558 is a potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer.

GSK3685032 is a time-independent, non-covalent, selective, and reversible DNMT1 inhibitor with an IC₅₀ of 0.036 μM. GSK3685032 induces loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth, and can be used in cancer therapy research.

Divarasib (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib irreversibly locks KRAS G12C oncoprotein in an inactive state and inhibits tumor cell growth. It is being investigated for use in solid tumors, including non-small cell lung and colorectal cancers and other types of cancer.

Arbutamine (GP 21213) is a novel potent non-selective beta-adrenoceptor agonist with alpha-1-sympathomimetic activity.Arbutamine promotes cardiac stress and increases heart rate, cardiac contractility.Arbutamine can be used to study cardiac stress and coronary artery disease

CF53 is a highly potent, selective, and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM, and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, being very selective over non-BET bromodomain-containing proteins. CF53 exhibits potent anti-tumor activity both in vitro and in vivo.

CFM-2, a potent and selective non-competitive antagonist of AMPAR (AMPAR), exhibits anticonvulsant activity across various seizure models.

DJ001 is a highly specific, selective, and non-competitive protein tyrosine phosphatase σ (PTPσ) inhibitor with an IC50 of 1.43 μM, and it promotes the regeneration of hematopoietic stem cells.

DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA αxβ3γ2 receptor subtypes. For α1, α2, α3, and α5 receptors, their Kis were 10 nM, 13 nM, 7.5 nM, 2.2 nM, respectively.

Giredestrant tartrate (Estrogen receptor antagonist 1) is a novel, orally active, selective and effective non-steroidal estrogen receptor antagonist. Giredestrant tartrate strongly binds to ER, resulting in the failure of ER to activate the transcription of targeted genes and promoting the degradation of ER protein. Giredestrant tartrate can be used to treat tumor diseases.

INT-777 (S-EMCA) is a potent, selective TGR5 agonist with an EC₅₀ of 0.82 μM. Following subarachnoid hemorrhage in rats, INT-777 inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3/cAMP/PKA signaling pathway. INT-777 exhibits multiple effects, including metabolic regulation, anti-inflammatory activity, cholagogue effects, and vascular protection. INT-777 can be used in research on diseases such as metabolic syndrome, non-alcoholic fatty liver disease, inflammatory bowel disease, and pulmonary arterial hypertension.

P053 is a potent, non-competitive, and selective ceramide synthase 1 (CerS1) inhibitor with an IC50 of 0.5 μM. It acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle and regulates whole-body adiposity[1].

Penbutolol sulfate ((-)-Terbuclomine) binds to both β2-adrenergic and β1-adrenergic receptors, making it a non-selective β-blocker.

(R)-Carvedilol is a non-selective blocker of β/α-1. (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).