Gutathione S-transferase

Glutathione S-transferases (GSTs) are a diverse group of phase II drug metabolizing enzymes whose shared function is the conjugation of glutathione (GSH) to various electrophilic endo- and xenobiotics. GSTs have been implicated in the conjugation of endogenously produced oxidized metabolites including propenal, 4-hydroxynonenals, organic hydroperoxides, phospholipids, and fatty acid peroxides.

On the basis of subcellular localization, the GST enzymes are grouped into three different classes namely, membrane-bound microsomal, mitochondrial and cytoplasmic. The leading and most diverse group of GSTs are the cytosolic enzyme spresent in humans. These are known as phase II detoxification enzymes that comprise of at least 8 classes of isoenzymes: alpha (A), kappa (K), mu (M), omega (O), pi (P), sigma (S), theta (T), and zeta (Z). In addition, four different classes of this superfamily, called beta (β), delta(δ), phi (Φ) and tau (τ) are also present in bacteria, insects and plants.

GSTs have emerged as a promising therapeutic target because specific isozymes are overexpressed in a wide variety of tumors and may play a role in the etiology of other diseases, including neurodegenerative diseases, multiple sclerosis, and asthma.

Gutathione S-transferase 相关产品（9）

货号	产品名	Cas	产品描述
PL02817	AZD9898	2042347-69-1	AZD9898 是一种口服有效的白三烯-C4 合成酶 (LTC4S) 抑制剂，IC50 值为 0.28 nM。AZD9898 减轻GABA 结合和肝毒性信号。AZD9898 可用于哮喘的研究。
PL05542	Ethacrynic acid	58-54-8	Ethacrynic acid (Etacrynic acid) 是一种利尿剂。Ethacrynic acid 是谷胱甘肽 S-转移酶 (GSTs) 的抑制剂。Ethacrynic acid 是一种 NF-κB 信号传导途径的有效抑制剂，并且还调节白三烯的形成。Ethacrynic acid 还可抑制 L 型电压依赖性和储存操作的钙通道，从而导致气道平滑肌细胞松弛。Ethacrynic acid 具有抗炎特性，可减轻类维生素 A 诱导的小鼠耳部水肿。
PC14914	Ezatiostat hydrochloride	286942-97-0	GST抑制剂，Ezatiostat(TER199; TLK199)盐酸盐是谷胱甘肽类似物，是谷胱甘肽s-转移酶（GST）P1-1抑制剂。
PL02052	GSTO-IN-2	1202710-57-3	GSTO-IN-2是一种谷胱甘肽S-转移酶 (glutathione S-transferase) 抑制剂，对于GSTA2，GSTM1和GSTP1-1的 IC50 值分别为3.6，16.3，1.4 μM。
PL01929	GSTO1-IN-1	568544-03-6	GSTO1-IN-1 是一种有效的谷胱甘肽 S-转移酶 omega 1 (GSTO1) 抑制剂，IC50 为 31 nM。
PC15305	Iberin(solution)	505-44-2	诱导II期解毒酶的表达，包括醌还原酶和谷胱甘肽S-转移酶，Iberin是萝卜硫素的亚砜类似物，是天然存在的异硫氰酸酯家族的成员。抑制HL60细胞的IC50值为2.3 μM。
PL02270	LAS17	2362527-67-9	LAS17 是一种强效的，不可逆的，选择性谷胱甘肽 S-转移酶 Pi (GSTP1) 抑制剂。LAS17 抑制 GSTP1 活性，IC50 为 0.5 µM.
PL02326	TK05	1245734-61-5	TK05 是一种有效选择性的白三烯 C4 合成酶 (LTC4S) 抑制剂，其 IC50 值为 95 nM。
PL03593	TLK117	152684-53-2	TLK197是TLK199的活性代谢物，选择性抑制谷胱甘肽S-转移酶P1-1 (Glutathione S-transferase P1–1 (GSTP1-1))，结合 GSTP的 Ki 值为0.4 μM。 TLK117还竞争性地抑制乙二醛酶I (glyoxalase I)， Ki值为0.56 μM。