a-163

Triaziquone is an alkylating agent that can react with DNA to form intrastrand crosslinks.

EM 163 is a TIR-TIR interaction inhibitor, which is a TIR (Toll/interleukin-1 receptor) structural domain mimic of the MyD88 protein. EM 163 targets the TIR structural domain in the IL-1 receptor and blocks the interaction with MyD88. EM 163 inhibits the production of inflammatory cytokines in vivo caused by staphylococcal enterotoxin B (SEB). EM 163 protects mice from SEB shock-induced death. In rat hippocampal neurons in vitro, EM 163 blocked the activation of p38 and the inhibitory effect of IL-1β on chemically induced long-term potentiation (LTP)-triggered protein synthesis.

NRX-103095 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP and enhances the affinity of pSer33/Ser37 β-catenin for β-TrCP with an EC50 of 163 nM.

Harman hydrochloride can directly induce CYP1A1 gene expression in an AhR-dependent manner and may represent a novel mechanism by which harman promotes mutagenicity, co-mutagenicity and carcinogenicity.

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

Ens-163 phosphate is a muscarinic M1 receptor agonist. It is selective.

Pomalidomide-PEG2-Oms is a conjugate of the E3 ligase ligand and linker, serving as a component of EGFR PROTAC DDC-01-163.

DDC-01-163 is a selective PROTAC degrader targeting EGFR mutants, with an IC50 of 45 nM.

JBJ-07-149 is an inhibitor of EGFRL858R/T790M with an IC50 of 1.1 nM. It suppresses the proliferation of Ba/F3 cells with IC50 values of 4.9 μM when used alone, and 0.148 μM when combined with Cetuximab. Additionally, JBJ-07-149 can serve as a target protein ligand for synthesizing [DDC-01-163].

E3 Ligase Ligand-linker Conjugate 163 is the E3 ligase ligand (E3 Ligase Ligand 58)-linker conjugate component of AH078, a PROTAC that selectively degrades CK1δ and CK1ε. It is utilized in research related to circadian rhythm disorders.

AH078 (compound 37) is a selective PROTAC degrader targeting CK1δ and CK1ε with low selectivity for CK1α. AH078 consists of a PROTAC linker (black part) Monomethyl octanoate, a target protein ligand (red part) CK1δ/CK1ε ligand-1, and an E3 ligase ligand (blue part) E3 Ligase Ligand 58. The E3 ligase ligand combined with the linker forms the conjugate E3 Ligase Ligand-linker Conjugate 163.

Antitumor agent-163 (Compound 3) serves as a photosensitizer in molecular-targeted photodynamic therapy (MT-PDT) aimed at carbonic anhydrase IX (CAIX). Under illumination at 540 nm, Antitumor agent-163 inactivates CAIX protein through singlet oxygen generation without affecting internal standard proteins such as α-tubulin, β-actin, and proliferating cell nuclear antigen (PCNA). It induces cell membrane damage and reduces cell viability with IC50 values of 0.2 μM for A549 and 0.05 μM for U87MG. Furthermore, Antitumor agent-163 demonstrates antitumor activity in mouse models.

EGFR-IN-163 (Compound 13) is a competitive inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.079 μM and selective inhibition on HER-2. It induces apoptosis in tumor cells and causes cell cycle arrest at the G₂/M phase. EGFR-IN-163 shows promise for investigating estrogen receptor-positive (ER+) breast cancer.

JP-163-16 is a RelA/p65 PROTAC degrader. It selectively reduces the expression of RelA/p65 in cells via a proteasome-dependent mechanism. JP-163-16 induces apoptosis by inhibiting the NF-κB signaling pathway. This compound is applicable for research on RelA/p65-dependent tumors, such as chronic lymphocytic leukemia (CLL).

MMH-165-26 is a ligand for the RelA/p65 protein. It reduces the expression of RelA/p65 and exhibits significant cytotoxicity in MEC-1 cells (LC50 = 0.37 μM). MMH-165-26 can be used in the synthesis of PROTACs, such as [JP-163-16].

β-Interleukin I (163-171), human Acetateis a peptide that participate in the regulation of immune responses, inflammatory reactions, and hematopoiesis.

163-bp3 is an effective photoaffinity probe and can be used as a target γ Secretory enzyme.

Harmane (Loturine) is a bio-active β-Carboline and monoamine oxidase inhibitor found in coffee and tobacco smoke.

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3',5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3'-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

JIP-1(153-163) TFA (TI-JIP TFA), a c-JNK peptide inhibitor derived from residues 153-163 of JNK-interacting protein-1 (JIP-1), features a modification at Phe-11 with a C-terminal amide [1].

Antibacterial agent 163 (compound 1), a hydroxyquinoline derivative, potently inhibits methicillin-resistant Staphylococcus aureus (MRSA) [1].

JIP-1(153-163) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). JIP-1(153-163) binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.

JIP-1 (153-163) acetate(438567-88-5 free base) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). JIP-1 (153-163) acetate(438567-88-5 free base) binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.

D-JBD19 [D-JNKI1-TAT (residues 153-163)] is a non-permeable peptide that offers neuroprotective effects.