s 130

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

Allitinib (AST-1306) 是可口服的 EGFR 和 ErbB2不可逆抑制剂，IC50分别为 0.5 和 3 nM。它具有抗癌活性，抑制 ErbB4，IC50为 0.8 nM。

NS13001 (N-(4-Chlorophenyl)-2-(3,5-dimethyl-1H-pyrazol-1-yl)-9-methyl-9H-purin-6-amine) 是口服有效的 SK 通道选择性正向变构调节剂。NS13001 对 SK2 和 SK3 通道的 EC50分别为 1.8 μM 和 0.14 μM。NS13001 在脊髓小脑共济失调 2 型和其他小脑共济失调方面具有研究价值。

KLS-13019 is a Cannabidiol-Derived Neuroprotective Agent with Improved Potency, Safety, and Permeability. (EC50=40nM; T1=7500). KLS-13019 was 50-fold more potent and >400-fold safer than cannabidiol and exhibited an in vitro profile consistent with imp

Macimorelin (EP-1572) acetate，一种 GH 促分泌素，是一种具有口服活性的GHSR 激动剂。Macimorelin acetate 可刺激 GH 的释放。Macimorelin acetate 可用于成人生长激素缺乏症 (AGHD) 和癌症厌食-恶病质综合征 (CACS) 的研究。

KISS1-305, the Metastin Kisspeptin analog, is a prototype peptide and chemical probe with suboptimal KISS1R agonistic activity and resistance to plasma protease degradation.

Navtemadlin (AMG232) 是一种有效的、选择性的、可口服的 p53-MDM2 相互作用抑制剂，IC50值为 0.6 nM。它以 0.045 nM 的 Kd 与 MDM2 结合。

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) 是一种有效的JAK1 2抑制剂。Ruxolitinib sulfate 抑制JAK1 2的IC50为 3.3 nM 2.8 nM，高于 JAK3 130 倍。

ZXH-4-130 TFA为高效、选择性CRBN降解剂，属于CRBN-VHL类(hetero-PROTAC)化合物。在MM1.S细胞中，10 nM ZXH-4-130 TFA可诱导约80%的CRBN降解。