a-1 protease inhibitor 5

SJB3-019A 是一种有效的、有效的和新型的泛素特异性蛋白酶1（USP1）抑制剂，在 K562细胞中促进 ID1降解和细胞毒性的作用是 SJB2-043的5倍，IC50为0.0781 μM。SJB3-019A 抑制细胞增殖，使细胞凋亡。

Rasagiline-13C3is intended for use as an internal standard for the quantification of rasagiline by GC- or LC-MS. Rasagiline is an inhibitor of monoamine oxidase B (MAO-B; IC50= 4.43 nM for the rat brain enzyme).1It is selective for MAO-B over MAO-A (IC50= 412 nM for the rat brain enzyme). It inhibits serum and NGF withdrawal-induced apoptosis of PC12 cells when used at concentrations ranging from 0.01 to 100 μM.2Rasagiline inhibits rat brain MAO-Bin vivo(ED50= 0.1 mg kg).1It reduces cerebral edema in a mouse model of traumatic brain injury.2Rasagiline (0.1 mg kg) reduces cortical and hippocampal levels of full-length and soluble amyloid precursor protein (APP) in rats and mice. It also reduces α-synuclein-induced substantia nigral neuron loss and improves motor dysfunction in a mouse model of Parkinson's disease.3Formulations containing rasagiline have been used in the treatment of Parkinson's disease. 1.Youdim, M.B.H., Gross, A., and Finberg, J.P.Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase BBrit. J. Pharmacol.132(2)500-506(2001) 2.Youdim, M.B.H., and Weinstock, M.Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R) aminoindan-5-YL)-ethyl methyl carbamate]Cell. Mol. Neurobiol.21(6)555-573(2001) 3.Kang, S.S., Ahn, E.H., Zhang, Z., et al.α-Synuclein stimulation of monoamine oxidase-B and legumain protease mediates the pathology of Parkinson's diseaseEMBO J.37(12)e98878(2018)

5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B NS3 protease inhibitor with an IC50 of 0.48 μg mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability[1]. [1]. Deng-wei Wu, et al. Policresulen, a novel NS2B NS3 protease inhibitor, effectively inhibits the replication of DENV2 virus in BHK-21 cells. Acta Pharmacol Sin. 2015 Sep;36(9):1126-36.

MALT1-IN-9 (WO2021000855A1, Compound 5), a highly potent inhibitor of MALT1 protease, demonstrates an IC50 value of <500 nM when tested in Raji MALT1-GloSensor cells. MALT1-IN-9 exhibits significant anticancer properties [1].

SARS-CoV-2 3CLpro-IN-5 是一种针对 3C样蛋白酶3CLpro 的共价抑制剂，其抑制活性的 IC50 为 3.8 nM。该化合物的口服生物利用度（BA）为 9.0%，可用于 COVID-19 研究。

HIV-1protease-IN-4 (Compound II-22) 是一种有效的HIV-1蛋白酶抑制剂。HIV-1protease-IN-4 是阿扎那韦的前体。HIV-1蛋白酶-IN-4 作为前体，与口服母体活性分子相比，将母体 1 输送到大鼠血浆中的 AUC 高 5 倍，C24 高 67 倍[1]。