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SR10067 is a potent, selective, and brain-penetrant agonist of Rev-Erbβ (IC50 = 160 nM) and Rev-Erbα (IC50 = 170 nM) with anxiolytic activity.

Prinaberel (ERB 041) is a selective and potent estrogen receptor β (ERβ) agonist with anticancer activity that restores or increases ERβ expression and reduces cancer cell proliferation in mouse squamous cell carcinoma and human carcinoma cells. Prinaberel exhibits anti-inflammatory activity, inhibits the NFκB pro-inflammatory signaling pathway, and induces apoptosis of ovarian cancer cells. study endometriosis.

Erb-196 is an estrogen receptor-receptor agonist with non-steroidal selectivity.

Autophagy/REV-ERB-IN-1 is a dual inhibitor of autophagy and REV-ERB. It exhibits antitumor activity, with a CC50 value of 2.3 μM in BTB-474 cells.

Autophagy/REV-ERB-IN-1 hydrochloride (Compound 24) is a dual inhibitor of autophagy and REV-ERB with anticancer properties. It enhances the efficacy of autophagy blockade and increases cytotoxicity against cancer cells. Autophagy/REV-ERB-IN-1 (hydrochloride) is applicable in melanoma research.

SR9009 (Stenabolic), a REV-ERB agonist, increases the constitutive repression of genes regulated by REV-ERBα/ERBβ (IC50: 670/800 nM). Through activation of REV-ERB, SR9009 can decrease circadian locomotor activity during the dark phase and alter the expression pattern of core clock genes in the hypothalami of mice. The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle, and adipose tissue was also altered in mice exposed to SR9009, resulting in increased energy expenditure. In Diet-induced obese mice, SR9009 (100 mg/kg, i.p., b.i.d., for 30 days) could decrease fat mass and markedly improve dyslipidemia and hyperglycemia.

SR8278 is an REV-ERBα antagonist(EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112

1-(2-Aminoethyl)-1H-pyrazol-4-ylphosphonic acid linker-BSA is a hapten-carrier protein conjugate formed by coupling 1-(2-Aminoethyl)-1H-pyrazol-4-ylphosphonic acid linker to bovine serum albumin (BSA). As a hapten, 1-(2-Aminoethyl)-1H-pyrazol-4-ylphosphonic acid linker alone cannot induce an immune response and must be conjugated to a large molecular protein to become a complete antigen with immunogenicity. 1-(2-Aminoethyl)-1H-pyrazol-4-ylphosphonic acid linker-BSA may be supplied as a lyophilized powder or as a solution. The solution is prepared in 0.01 M TBS (pH 7.4) buffer at a typical concentration of 1 mg/mL.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

SBE-β-CD (Sulfobutylether-β-Cyclodextrin) is a β-cyclodextrin derivative with a sodium sulfonate salt separated from the lipophilic cavity by a butyl ether spacer group, or sulfobutylether. SBE-β-CD is widely used as a co-solvent in biological experiments.

Glyphosate (Atila) is an herbicide. It also is a possible carcinogen to humans.

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

NSC 228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulating EGFR tyrosine phosphorylation.

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase with IC50 values of 5.3 nM for drug-resistant mutant EGFR T790M and 8.3 nM for WT EGFR kinases.

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

Pyrotinib dimaleate is a selective EGFR/HER2 dual inhibitor with IC50 values ​​of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.

Terbufibrol reduces the levels of serum total cholesterol in normal and hypercholesterolemic male rats.

PF-06459988 is a novel, effective, orally active, irreversible, and selective epidermal growth factor receptor (EGFR) mutant inhibitor. PF-06459988 has high efficiency and high affinity for EGFRs double mutants containing T790M, and has minimal activity against WT EGFR. PF-06459988 makes a candidate drug for the treatment of cancer.

Terbogrel is an oral thromboxane A2 receptor antagonist (IC50 is about 10 nM) and thromboxane A2 synthase inhibitor (IC50 is about 10 nM). Terbogrel is an antiplatelet compound that inhibits platelet aggregation and is a potential compound for the prevention of blood clots.

Erbulozole (R 55104) is a potent synthetic microtubule inhibitor with anti-invasive, anti-tumor, and radiosensitizing activities that induces Wernicke's encephalopathy-like neurotoxicity.

Sudoterb free base (Sudoterb) , also known as LL3858, is an anti-tubercular drug candidate.

Berberine ursodeoxycholate (HTD1801) is an orally effective hypolipidemic agent, an ionic salt of Berberine and Ursodeoxycholic acid.Berberine ursodeoxycholate has a wide range of metabolic activity and significantly reduces liver fat content. Berberine ursodeoxycholate has been used in studies of hyperlipidemia, non-alcoholic steatohepatitis (NASH) and diabetes.

EGFR/ErbB-2 inhibitor-1 is a selective ErbB2/HER2 inhibitor that effectively blocks ErbB2 and HER2 signaling.