GlpBio

Proteases

Proteases(蛋白酶)

Proteases, also known as peptidases or proteolytic enzymes, consists of a large number of enzymes catalyzing the hydrolysis of peptide bonds and subsequently resulting in the degradation of protein substrates into amino acids. Proteases are involved in a wide range of human diseases, including cancer, neurodegenerative disorders, inflammatory diseases and cardiovascular diseases. Thus numerous proteases inhibitors (small molecules and proteins) have been identified to block activity of proteases. Proteases inhibitors can be classified into different types based on the class of proteases they inhibit through two general mechanisms, irreversible “trapping” reactions and reversible tight-binding reactions. Proteases inhibitors have been used as diagnostic or therapeutic agents for the treatment of proteases-related diseases.

研究方向

Proteases 相关产品(4079)

  • GC63237 structure
    GC63237trans-3-Indoleacrylic acid
    CAS: 29953-71-7
    纯度: >98.00% / >95.00%

    trans-3-Indoleacrylic acid is a metabolite of tryptophan.

  • GC63238 structure
    GC63238Tricarballylic acid
    CAS: 99-14-9
    纯度: >98.00%

    Tricarballylic acid (β-Carboxyglutaric acid, Propane-1,2,3-tricarboxylic acid) is an inhibitor of aconitase and therefore interferes with the Krebs cycle.

  • GC63256 structure
    GC63256VRT-043198
    CAS: 244133-31-1
    纯度: >98.00%

    VRT-043198 是 VX-765 (Belnacasan) 的活性代谢物，是有效的、选择性的、能透过血脑屏障的 caspase-1 的抑制剂。VRT-043198 对 caspase-1 和 caspase-4 的 Ki 值分别为 0.8 nM 和 0.6 nM。

  • GC63275 structure
    GC63275β-Cryptoxanthin
    CAS: 472-70-8
    纯度: >96.50%

    β-Cryptoxanthin ((3R)-β-Cryptoxanthin) 是从萨摩橘中分离的一种含氧类胡萝卜素，也是有效的抗氧化剂。β-Cryptoxanthin 具有抗应激作用。

  • GC63279 structure
    GC63279γ-Glu-Gly TFA

    γ-Glu-Gly 是一种 γ-谷氨酰二肽，是一种人体脂质代谢物。γ-Glu-Gly 与 GABA (γ-氨基丁酸)结构相似，可作为兴奋性氨基酸的拮抗剂。

  • GC63282 structure
    GC63282Icapamespib
    CAS: 1000999-96-1

    Icapamespib (PU-HZ151) 是一种有效的 HSP90 抑制剂，EC50 值为5 nM. Icapamespib 可以透过血脑屏障。

  • GC63311 structure
    GC63311Omeprazole metabolite Omeprazole sulfone (methoxy-d3)
    CAS: 1189891-71-1

    Omeprazole metabolite Omeprazole sulfone (methoxy-d3) (Omeprazole sulfone (methoxy-d3)) 是 Omeprazole metabolite Omeprazole sulfone 的氘代物。Omeprazole sulfone是Omeprazole的代谢物。

  • GC63319 structure
    GC63319Ercalcidiol-d3
    CAS: 1217467-39-4
    纯度: >99.00%

    Ercalcidiol-d3 (25-hydroxy Vitamin D2-d3) 是 Ercalcidiol 的氘代物。Ercalcidiol 是维生素 D2 的代谢产物。Ercalcidiol 可用作维生素 D 状态的指标。

  • GC63322 structure
    GC63322MMP13-IN-3
    CAS: 1222173-37-6

    An inhibitor of MMP-13

  • GC63337 structure
    GC63337N-Acetyl Norgestimate-d6
    CAS: 1263195-02-3
  • GC63338 structure
    GC63338GCPII-IN-1 TFA
    CAS: 1269794-89-9

    GCPII-IN-1 TFA 是一种谷氨酸羧肽酶 II (GCPII; PSMA) 抑制剂支架，Ki 为 44.3 nM。

  • GC63342 structure
    GC63342Quinaprilat-d5
    CAS: 1279034-23-9
    纯度: >91.00%

    Quinaprilat-d5 是一种 Quinaprilat 氘代物。Quinaprilat 是一种非巯基 ACE 抑制剂，是Quinapril 活性代谢物。Quinaprilat 特异性阻断血管紧张素 I 向血管收缩剂血管紧张素 II 的转化，并抑制缓激肽的降解。Quinaprilat 主要作为血管扩张剂，降低外周和肾血管的总阻力。

  • GC63352 structure
    GC63352Ebaresdax
    CAS: 1334471-39-4
    纯度: >99.50%

    Ebaresdax对SIN-1诱导的过氧亚硝酸盐氧化和过氧亚硝酸盐介导的细胞毒性均有抑制作用，IC50s分别为3.7±0.80和0.13±0.02 uM。

  • GC63363 structure
    GC63363M435-1279
    CAS: 1359431-16-5

    M435-1279 is a UBE2T inhibitor, inhibiting the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.

  • GC63366 structure
    GC63366Fosciclopirox
    CAS: 1380539-06-9

    Fosciclopirox(CPX-POM) selectively delivers the active metabolite, Ciclopirox (CPX) that targets γ-secretase complex (Presenilin 1 and Nicastrin)2. It is used in the treatment of urothelial cancer and a number of solid and hematologic malignancies.

  • GC63383 structure
    GC63383Sitagliptin-d4 phosphate
    CAS: 1432063-88-1

    Sitagliptin-d4 (MK-0431-d4) phosphate 是 Sitagliptin phosphate 的氘代物。Sitagliptin phosphate (MK-0431 phosphate) 是一种有效的 DPP4 抑制剂，在 Caco-2 细胞中，IC50 值为 19 nM。

  • GC63389 structure
    GC63389DP-1
    CAS: 1472616-61-7
    纯度: >99.50%

    DP-1 是 SDC-TRAP-0063 的降解产物，是 Ganetespib 的一个片段。Ganetespib 是一种具有抗肿瘤活性的热休克蛋白 90 (HSP90) 抑制剂。

  • GC63399 structure
    GC63399HIV-1 integrase inhibitor 8
    CAS: 1568-80-5

    HIV-1 integrase inhibitor 8 是 HIV-1 整合酶 (HIV-1 integrase) 抑制剂，化合物 8。

  • GC63407 structure
    GC63407PF-06648671
    CAS: 1587727-31-8
    纯度: >98.00%

    PF-06648671 是一种新型的，可通透血脑屏障的，具有口服活性的 γ 分泌酶 (γ‐Secretase) 调节剂 (GSM)。PF-06648671 减少 Aβ42 和 Aβ40，并且伴随 Aβ37 和 Aβ38 的增加。PF-06648671 用于阿尔茨海默病的研究。

  • GC63423 structure
    GC63423Inclisiran
    CAS: 1639324-58-5

    Inclisiran (ALN-PCSsc) 是一种双链小干扰 RNA (siRNA) 分子，可抑制 PCSK-9 的转录。Inclisiran 可用于高脂血症和心血管疾病 (CVD) 研究。

  • GC63435 structure
    GC63435LTA4H-IN-1
    CAS: 1799681-85-8
    纯度: >98.50%

    An inhibitor of LTA 4 hydrolase

  • GC63467 structure
    GC63467Hydroxypyruvic acid lithium hydrate
    CAS: 209728-15-4

    Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) 是甘氨酸、丝氨酸和苏氨酸代谢的中间产物 (intermediate)。Hydroxypyruvic acid lithium hydrate 是丝氨酸-丙酮酸氨基转移酶和乙醛酸还原酶/羟基丙酮酸还原酶的底物 (substrate)。Hydroxypyruvic acid lithium hydrate 参与了二甲基甘氨酸脱氢酶缺乏症的代谢紊乱途径。

  • GC63481 structure
    GC63481Succinic acid-d6
    CAS: 21668-90-6

    Succinic acid-d6 (Wormwood acid-d6) 是 Succinic acid 的氘代物。Succinic acid 是三羧酸循环的中间产物，也是无氧代谢的发酵产物之一。

  • GC63497 structure
    GC63497Pedalitin
    CAS: 22384-63-0

    Pedalitin 是酪氨酸酶（IC50=0.28 mM）和α-葡萄糖苷酶抑制剂（IC50=0.29 mM）。