glutathione s-transferase a-1

Canfosfamide Hydrochloride 是一种改性谷胱甘肽类似物的盐酸盐，具有潜在的抗肿瘤活性。canfofamide 可被谷胱甘肽s -转移酶P1-1选择性激活，转化为与肿瘤细胞DNA 亲核中心形成共价键的烷基化代谢物，从而诱导细胞应激反应和细胞毒性，减少肿瘤增殖。

Oltipraz (RP 35972) 是一种 Nrf2的强效激活剂。它时间依赖性地抑制 HIF-1α激活，IC50为 10 μM，浓度 ≥ 10 μM 时完全消除 HIF-1α诱导。

Thonningianin A 是从非洲草药通宁宁的甲醇提取物中，分离得到的一种鞣花素，具有抗癌和抗氧化性，涉及自由基清除、抗超氧化物形成和金属螯合。

S-Methylglutathione (S-Methyl glutathione) 是一种 S 取代的谷胱甘肽，是一种转移酶A催化的1-氯-2,4-二硝基苯偶联物的抑制剂，也是一种 XOCl 清除剂。S-Methylglutathione 抑制乙二醛酶 1 (glyoxalase 1) ，诱导水螅触手球形成。

Ezatiostat hydrochloride (TLK199 HCl) 是一种新型谷胱甘肽类似物，可刺激淋巴细胞生成和骨髓祖细胞增殖，可用于治疗血细胞减少症和研究骨髓增生异常综合症。它也是口服活性的选择性谷胱甘肽 S-转移酶 P1-1 抑制剂，通过抑制 GSTP1导致 JNK 激活。

NBDHEX 是一种谷胱甘肽 S-转移酶 P1-1 抑制剂，也是晚期自噬抑制剂。它诱导肿瘤细胞凋亡，通过抑制 GST 的催化活性，避免抑制剂被特异性泵从细胞中排出，以及破坏 GSTP1-1和关键信号传导因子之间的相互作用，从而起到抗癌的作用。

GSTO-IN-2 是一种谷胱甘肽S-转移酶 （GST）抑制剂，抑制 GSTA2，GSTM1和 GSTP1-1，可用于研究肿瘤。

Protectin conjugates in tissue regeneration 1 (PCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid . DHA is oxidized to 16S,17S-epoxy-protectin, which is then converted to PCTR1 by glutathione S-transferase. PCTR1 levels increase during resolution of acute microbial-induced peritonitis in mice. PCTR1 (30 ng, i.p.) administration 12 hours post-infection increases macrophage numbers and activity and shortens the resolution phase of inflammation by 57%. It also reduces the levels of PGE2 , PGD2 , and TXB2 in peritoneal exudates.

Maresin conjugates in tissue regeneration 3 (MCTR3) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages. DHA is oxidized to maresin 1 , which is converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase, then to MCTR2 by γ-glutamyl transferase, and to MCTR3 by dipeptidase. MCTR3 accelerates tissue regeneration in planaria (1 and 100 nM) approximately as potently as MCTR2 and more potently than MCTR1. Pretreatment with MCTR3 prior to E. coli administration in mice reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR3 selectively reduces the amount of the eicosanoids PGD2 , PGE2 , PGF2α , and TXB2 in the exudate.

Maresin conjugates in tissue regeneration 1 (MCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages at the site of inflammation. DHA is oxidized to maresin 1 , which is then converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase. MCTR1 accelerates tissue regeneration in planaria (1 and 100 nM). Pretreatment with MCTR1 (50 ng mouse, i.p.) prior to E. coli administration reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR1 reduces the amount of eicosanoids in the exudate.

Canfosfamide (TLK-286) 是一种谷胱甘肽类似物前体药物，由谷胱甘肽 S-转移酶 P1-1 激活，诱导细胞凋亡 (apoptosis)。Canfosfamide 还抑制 DNA 依赖性蛋白激酶 (DNA-PK) 的催化激酶活性。Canfosfamide 在活化后产生一种抗癌烷基化剂和谷胱甘肽衍生物。Canfosfamide 可用于恶性肿瘤的研究。

Fraxinellone 是从白鲜的根皮中分离出来的一种天然产物，是PD-L1抑制剂，可抑制HIF-1α蛋白质合成。它通过靶向 PD-L1，有用于癌症免疫的潜力。

GSTP1-1 inhibitor 1 (compound 6b) 是一种不可逆且长效的谷胱甘肽转移酶 (Gutathione S-transferase) 抑制剂，专门针对 GSTP1-1，其 IC50 值为 21 μM。作为关键的抑癌靶标，GSTP1-1 inhibitor 1 显示出潜在的抗癌活性。

Curzerene，一种来自Curculigo orchioides Gaertn根茎的倍半萜化合物，具有强大的抗癌特性。它已知能够诱导细胞凋亡[1]并抑制谷胱甘肽S-转移酶A1（GSTA1）mRNA和蛋白质的表达。

Ezatiostat TFA (TLK199) 是一种具有造血刺激活性的谷胱甘肽 S-转移酶 (GST) P1-1 的脂质体小分子谷胱甘肽类似物抑制剂。

GSTO1-IN-1 是谷胱甘肽 S-转移酶 omega 1 抑制剂，IC50=31 nM。

Benastatin A is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2,3It inhibits glutathione S-transferase (GST; Ki= 5 μM for the rat liver enzyme).2Benastatin A is active against several bacteria, including methicillin-resistantS. aureus(MRSA; MIC = 3.12 μg ml). It induces apoptosis and cell cycle arrest at the G1 G0phase in Colon 26 mouse colon cancer cells when used at concentrations of 20 and 16 μM, respectively.3 1.Xu, Z., Schenk, A., and Hertweck, C.Molecular analysis of the benastatin biosynthetic pathway and genetic engineering of altered fatty acid-polyketide hybridsJ. Am. Chem. Soc.129(18)6022-6030(2007) 2.Aoyagi, T., Aoyama, T., Kojima, F., et al.Benastatins A and B, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. I. Taxonomy, production, isolation, physico-chemical properties and biological activitiesJ. Antibiot. (Tokyo)45(9)1385-1390(1992) 3.Kakizaki, I., Ookawa, K., Ishikawa, T., et al.Induction of apoptosis and cell cycle arrest in mouse colon 26 cells by benastatin AJpn. J. Cancer Res.91(11)1161-1168(2000)

S-Octylglutathione 是一种针对谷胱甘肽硫转移酶 (GST) 的竞争性抑制剂。

Maresin conjugates in tissue regeneration 2 (MCTR2) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages at the site of inflammation. DHA is oxidized to maresin 1 , which is converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase then to MCTR2 by γ-glutamyl transferase. MCTR2 accelerates tissue regeneration in planaria (1 and 100 nM). Pretreatment with MCTR2 prior to E. coli administration reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR2 selectively reduced the amount of the eicosanoids PGD2 and PGF2α in the exudate.

Benastatin C is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2It inhibits glutathione S-transferase (GST; IC50= 24 μg ml for the rat liver enzyme).2Benastatin C also inhibits the esterase activity of isolated porcine pancreatic lipase (IC50= 10 μg ml). It increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner. 1.Xu, Z., Schenk, A., and Hertweck, C.Molecular analysis of the benastatin biosynthetic pathway and genetic engineering of altered fatty acid-polyketide hybridsJ. Am. Chem. Soc.129(18)6022-6030(2007) 2.Aoyama, T., Kojima, F., Yamazaki, T., et al.Benastatins C and D, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. Production, isolation, structure determination and biological activitiesJ. Antibiot. (Tokyo)46(5)712-718(1993)

GST-IN-1 (compound 16) 为一种谷胱甘肽 S-转移酶 (GST) 抑制剂，其半抑制浓度 (IC50s) 分别针对sjGST为1.55 μM，针对hGSTM2为2.02 μM。

Cyclopropenone probe 1 可以通过在催化活性位点共价结合，特异且有效地修饰三阴性乳腺癌驱动因子 GSTP1。

Keap1-Nrf2-IN-9（compound 11）是一种有效Keap1-Nrf2PPI抑制剂，IC50为0.575 µM。该化合物能够提升Nrf2靶基因表达，涉及血红素加氧酶1 (Hmox1)、谷胱甘肽S转移酶P (GstP) 以及谷氨酸-半胱氨酸连接酶的催化(Gclc)与调节(Gclm)亚基。在ARPE19细胞中，Keap1-Nrf2-IN-9展现出无细胞毒活性。