s 130

S130 is a high affinity, selectiveATG4B (a major cysteine protease) inhibitor (IC50 of 3.24 μM).It suppresses autophagy flux.

KLS-13019 is a highly effective and orally active GPR55 receptor antagonist, a cannabidiol (CBD)-derived neuroprotective agent that can reverse chemotherapy-induced peripheral neuropathy (CIPN) and is suitable for studying hepatic encephalopathy (HE).

Allitinib (AST-1306) (AST-1306) has anti-cancer activity,and it is an irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. [1]

Thiophos (GS-13006) is an insecticide, which is an organic phosphate ester.

CTS-1027 is a small molecule inhibitor of MMPs (IC50s: 0.3 nM, 0.5 nM for MMP2, MMP13). It has > 1,000 fold selectivity over MMP1.

NS13001 (N-(4-Chlorophenyl)-2-(3,5-dimethyl-1H-pyrazol-1-yl)-9-methyl-9H-purin-6-amine) is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.

RS130-180 is a β-arrestin-biased agonist that selectively targets the 5-hydroxytryptamine 2A receptor (5-HT2aR). It shows promise for research in neuropsychiatric disorders such as depression.

Macimorelin Acetate (EP-1572), an orally active growth hormone (GH) secretagogue and a ghrelin receptor (GHSR) agonist, stimulates GH release. It is utilized in research focusing on adult growth hormone deficiency (AGHD) and Cancer Anorexia-Cachexia Syndrome (CACS).

KISS1-305, the Metastin/Kisspeptin analog, is a prototype peptide and chemical probe that resists plasma protease degradation but has suboptimal KISS1R agonistic activity in vitro.

Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.

S-Nitrosothiols (RSNOs) are a class of molecules that function as exogenous and endogenous nitric oxide (NO) donors. RSNOs found in vivo include proteins such as S-nitrosohemoglobin and S-nitrosoalbumin, as well as low molecular weight species such as S-nitrosoglutathione (GSNO) and S-nitrosocysteine (CysNO). CAY10565 is a member of a new class of S-nitrosothiol species that act as NO donors under acidic conditions. It decomposes with a half-life of 130 minutes in 0.1 M phosphate buffer, pH 5.0, at 37°C and relaxes phenylephrine-constricted rat aortic strips 71% and 44% at pH 6.0 and 7.4, respectively.

Streptazolin is a fungal metabolite originally isolated from S. viridochromogenes. It increases NF-κB activity when used at concentrations ranging from 60 to 130 μg/ml, at least in part, via PI3K signaling. Streptazolin enhances TNF-α secretion induced by LPS and enhances IL-8 secretion when used alone or in combination with LPS in THP-1 Blue cells.

Ruxolitinib sulfate (INCB018424 sulfate) is a potent, selective inhibitor of JAK1/2 with IC50 values of 3.3 nM/2.8 nM, demonstrating over 130-fold selectivity for JAK1/2 compared to JAK3.

ZXH-4-130 TFA is a hetero-PROTAC (CRBN-VHL compound) that efficaciously and selectively mediates the degradation of CRBN, achieving approximately 80% degradation at a concentration of 10 nM in MM1.S cells [1].