123-i

Adam I-123 is a radiopharmaceutical containing the serotonin transporter (SERT) ligand, with SERT-binding and radioisotope activities. SERT is a monoamine transporter protein found in the membranes of neurons and platelets.

Iobenguane I 123 is a bioactive chemical.

Iofolastat I 123 is a diagnostic agent under investigation in clinical trial NCT00992745 (A Phase I Pilot Study in Subjects With Metastatic Prostate Cancer).

MIP-1095 I-123, as a radiotracer, is under investigation in clinical trial NCT00712829 (Evaluating the Safety, Pharmacokinetics, Tissue Distribution, Metabolism and Dosimetry of Two Prostate Cancer Imaging Agents).

Selisistat (EX-527) is a potent and specific inhibitor of the deacetylase SIRT1 (IC50 = 38 nM) and can be utilized in the study of neurological disorders such as Huntington's chorea.

N-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea is a potent TRPV1 antagonist, blocking activation of TRPV1 by capsaicin with the IC50 of 123 nM.

Acitemate(Chinoin 123) has an inhibitory effect on atherosclerosis and reduces the permeability of the aorta in rabbits fed a hyperlipidemic diet, which can be used to study atherosclerosis.

KDM4-IN-2 is a potent and selective KDM4 KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.

SC-514 (GK 01140) is a selective, orally active, ATP-competitive IKK-2 inhibitor (IC50=11.2±4.7 μM), obstructs NF-κB-dependent gene expression.

WWL123 is a potent and selective ABHD6 inhibitor (IC50=430 nM). WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6 2 mice.

LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-6 is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM.

Rotigaptide is a novel and specific modulator of Cx43 and is a potent AAP. Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress.

EGFR-IN-123 (compound D06) is an effective EGFR inhibitor. It exhibits inhibitory activity against several cell lines including PC-9G, A549, A431, and HCT116, with IC50 values of 0.74, 1.36, 1.20, and 2.53 μM respectively.

SILA-123, an inhibitor of FLT3 (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM), induces cell apoptosis by hindering the cell cycle progression at the G0 G1 phase through the suppression of FLT3 phosphorylation and its downstream signaling pathways. This compound is utilized in the study of acute myeloid leukemia.

Antifungalagent 123 (Compound 4b) demonstrates strong affinity for the oxidoreductase of Staphylococcus aureus or membrane proteins of Candida albicans, exhibiting both antibacterial and antifungal properties. Additionally, it is capable of scavenging free radicals, showcasing antioxidant effects. Antifungalagent 123 also inhibits the TLR signaling pathway and possesses anti-inflammatory activity.

Tyrphostin 63 (compound 13) is an epidermal growth factor receptor (EGFR) inhibitor, with an IC50 of 375 μM and a Ki of 123 μM.

PROTAC CG167 is a potent and selective PROTAC degrader of CypA. It degrades CypA in a dose-dependent manner in Jurkat cells, with a DC50 of 123 nM. Additionally, PROTAC CG167 exhibits antiviral activity by inhibiting HIV-1 and HCV. (Pink: CypA Ligand; Black: Linker; Blue: E3LigaseLigand)

Fluindione is a hematologic drug.

Sdz 280 446 is one of the most active cyclopeptolide of many resistance-modifying agents in restoring rhodamine-123 retention within multidrug-resistant P388 cells.

Flavone glycoside from Robinia with antibacterial and diuretic properties; derived from kaempferol.The ability of robinin to reverse the multidrug resistance of the human colon cancer cell line Colo 320 expreβing MDR1 LRP was explored by monitoring their uptake of Rhodamine 123, but was shown to have minimal effect. Robinin (NSC-9222) was detected in lysates of the human breast cancer cell line MCF-7 using liquid chromatography-tandem maβ spectrometry.

Mesoridazine (thioridazine EP impurity B) is a phenothiazine antipsychotic with effects similar to chlorpromazine.

Negative control for BSJ-03-123 . Displays binding and no degradation of Cdk6 in vitro. Brand et al (2019) Homolog-selective degradation as a strategy to probe the function of CDK6 in AML. Cell Chem.Biol. 26 300 PMID:30595531

(±)10-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro.[1][2] It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes.[3][4][5] (±)10-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid. Reference:[1]. VanRollins, M., and Murphy, R.C. Autooxidation of docosahexaenoic acid: Analysis of ten isomers of hydroxydocosahexaenoate. J. Lipid Res. 25(5), 507-517 (1984).[2]. Reynaud, D., Thickitt, C.P., and Pace-Asciak, C.R. Facile preparation and structural determination of monohydroxy derivatives of docosahexaenoic acid (HDoHE) by α-tocopherol-directed autoxidation. Anal. Biochem. 214(1), 165-170 (1993).[3]. VanRollins, M., Baker, R.C., Sprecher, H., et al. Oxidation of docosahexaenoic acid by rat liver microsomes. J. Biol. Chem. 259(9), 5776-5783 (1984).[4]. Yamane, M., Abe, A., and Yamane, S. High-performance liquid chromatography-thermospray mass spectrometry of epoxy polyunsaturated fatty acids and epoxyhydroxy polyunsaturated fatty acids from an incubation mixture of rat tissue homogenate. J. Chromatogr. 652(2), 123-136 (1994).[5]. Kim, H.Y., Karanian, J.W., Shingu, T., et al. Sterochemical analysis of hydroxylated docosahexaenoates produced by human platelets and rat brain homogenate. Prostaglandins 40(5), 473-490 (1990).

AAK1-IN-1 (example 123) is an AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2.2 nM. AAK1-IN-1 can be used for neurodegenerative diseases research[1]. Adaptor associated kinase 1 (AAK1) is a member of the Arkl Prkl family of serine threonine kinases. AAKl mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAKl is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAKl modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis[1]. [1]. Guanglin Luo, et al. Biaryl kinase inhibitors. WO2015153720A1.