aldehyde dehydrogenase (aldh)

Disulfiram (TETD) 是一种乙醛脱氢酶 ALDH 的抑制剂，抑制 hALDH1 和 hALDH2 (IC50=0.15 1.45 μM)，具有特异性。Disulfiram 对酒精产生急性敏感性，还可以抑制 GSDMD 孔形成。

3-Hydroxybenzaldehyde 是很多酚类化合物的前体分子。它是人和大鼠醛脱氢酶 (ALDH) 的底物 (substrate)。它具有血管保护的作用。

4-Diethylaminobenzaldehyde 是醛脱氢酶(ALDHs)的可逆抑制剂，对 ALDH1 的 Ki 为 4 nM，具有较强的抗雄激素作用 ，IC50为1.71 μM。

Win 18446 是口服有效的睾丸特异性的ALDH1a2的抑制剂，IC50为 0.3 μM。Win 18446 抑制睾丸内视黄醇合成视黄酸，可逆的抑制多个物种的精子形成，。

Dyclonine hydrochloride (Dyclonine HCl) 是润喉片的有效成分，具有显著的杀菌和杀真菌作用。

4-Hydroxynonenal (4-HNE) 是一种 α，β 不饱和羟基烯醛，可作为氧化 亚硝化应激生物标志物。它是ALDH2的底物和抑制剂。它可以调节许多信号传导过程，主要是通过与蛋白质，核酸和膜脂质中具有亲核官能团的共价加合物形成的。它通过线粒体在癌症中起重要作用。

Prunetin (Prunusetin) 是一种O-甲基化异黄酮，具有抗炎的作用。它是人醛脱氢酶的有效抑制剂。

Taraxerone 是分离自景天的天然产物。它可以增强乙醇脱氢酶和乙醛脱氢酶活性，EC50分别为 512.42 μM 和 500.16 μM。

NCT-501 是一种茶碱类化合物，有效抑制醛脱氢酶 1A1(ALDH1A1), 抑制 hALDH1A1 IC50为 40 nM, 选择性超过其它 ALDH 同工酶和其它脱氢酶 (作用于 hALDH1B1, hALDH3A1, 和 hALDH2 时,IC50值 >57 UM)。

CM10是一种有效的乙醛脱氢酶 1A (ALDH1A) 家族选择性抑制剂，对于 ALDH1A1，ALDH1A2 和 ALDH1A3 的IC50分别为 1700、740 和 640 nM。CM 10 可以调节新陈代谢并具有抗癌活性。

NCT-505是乙醛脱氢酶的选择性抑制剂，IC50为 7 nM。对 hALDH1A2，hALDH1A3，hALDH2，hALDH3A1的抑制作用较弱，IC50分别为 >57，22.8，20.1，>57 μM。

CVT-10216 是可逆的、选择性的醛脱氢酶 2（ALDH-2）抑制剂，IC50为 29 nM。对 ALDH-1的抑制作用较弱，IC50为 1.3 μM。 它可以减少偏爱酒精的大鼠过量饮酒，并表现出抗焦虑作用。

Alda-1是一种 ALDH2 激动剂，是野生型 ALDH2*1 和亚洲 E487K 突变体 ALDH2*2 形式的线粒体醛脱氢酶 2 的细胞渗透激活剂。

MeDTC (S-Methyl-N,N-diethylthiocarbamate Sulfone), 作为 Disulfiram 的一种代谢产物，它是一种高效的不可逆 ALDH (醛脱氢酶) 抑制剂。

BODIPY aminoacetaldehyde (BAAA) 是醛脱氢酶（ALDH）的荧光底物，可根据 ALDH 活性分离人类造血干细胞。

CM39 is an ALDH inhibitor. Aldehyde dehydrogenase (ALDH) activity is commonly used as a marker to identify cancer stem-like cells. The three ALDH1A isoforms have all been individually implicated in cancer stem-like cells and in chemoresistance.

ALDH1A1-IN-4 (compound A1) 作为一种有效的乙醛脱氢酶 (ALDH) A1 抑制剂，其IC50为 0.32 μM，对癌症研究具有重要意义。

BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the efflux pump P-glycoprotein (P-gp) but co-application of BAAA with a P-gp inhibitor, such as verapamil , inhibits BAA efflux.2BAAA-DA has been used to isolate human hematopoietic progenitor cells, which have high ALDH activity, andviaflow cytometry to sort cancer stem cells that contain high levels of ALDH.1,3BAA used in cells can be excited at 488 nm and displays an emission maximum of 512 nm.4 1.Storms, R.W., Trujillo, A.P., Springer, J.B., et al.Isolation of primitive human hematopoietic progenitors on the basis of aldehyde dehydrogenase activityProceedings of the National Academy of Sciences of the United States of America96(16)9118-9123(1999) 2.Smith, C.A., Colvin, M., Storms, R.W., et al.BODIPY aminoacetaldehyde diethyl acetal08010501.81-15(2010) 3.Leng, Z., Yang, Z., Li, L., et al.A reliable method for the sorting and identification of ALDHhigh cancer stem cells by flow cytometryExp. Ther. Med.(2017) 4.Pomper, M.G., Wang, H., Minn, I., et al.Red fluorescent aldehyde dehydrogenase (ALDH) substrate(2015)

Aldehyde dehydrogenaseNAD(P) (ALDH) 催化醛氧化成相应的羧酸，伴随辅因子 NAD(P) 还原成 NAD(P)H，常用于生化研究。Aldehyde dehydrogenaseNAD(P) 是人体用来缓解乙醛应激的许多酶系统之一。

DOPAL is an aldehyde product of the oxidative deamination of dopamine by monoamine oxidase.[1] It can be further oxidized to 3,4-dihydroxyphenylacetic acid (DOPAC) by aldehyde dehydrogenase (ALDH) and, to a lesser extent reduced to 3,4-dihydroxyphenyl ethanol (DOPET). DOPAL is toxic to neurons.[2],[3] It can also oligomerize and precipitate α-synuclein, an event associated with Parkinson's disease.[2] Mice lacking cytosolic and mitochondrial forms of ALDH display increased levels of DOPAL as well as neurodegeneration and motor dysfunction characteristic of Parkinson’s disease.[4]

11-Dehydro-2,3-dinor Thromboxane B2 (11-dehydro-2,3-dinor TXB2) is a metabolite derived from the inactive TXA2 metabolite, TXB2. Its formation involves the action of cytosolic aldehyde dehydrogenase (ALDH) and β-oxidation processes. Remarkably, levels of 11-dehydro-2,3-dinor TXB2 have been observed to increase by 5.2-fold in a surgery-induced rat model of tendon overuse, highlighting its potential role in physiological stress responses.

Methyl diethyldithiocarbamate is an active metabolite of the aldehyde dehydrogenase inhibitor disulfiram .1It is produced by methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes.2Methyl diethyldithiocarbamate inhibits liver low Kmaldehyde dehydrogenase (ALDH) in rats (ID50= 15.5 mg/kg).1It decreases mean arterial pressure (MAP) and increases heart rate during ethanol challenge in rats when administered at a dose of 20.6 mg/kg. 1.Hart, B.W., Yourick, J.J., and Faiman, M.D.S-methyl-N,N-diethylthiolcarbamate: A disulfiram metabolite and potent rat liver mitochondrial low Km aldehyde dehydrogenase inhibitorAlcohol7(2)165-169(1990) 2.Gessner, T., and Jakubowski, M.Diethyldithiocarbamic acid methyl ester. A metabolite of disulfiramBiochem. Pharmacol.21(2)219-230(1972)

NCT-501 hydrochloride is a highly potent and selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), which is based on theophylline. It effectively inhibits hALDH1A1 with an IC50 value of 40 nM, exhibiting superior selectivity towards hALDH1A1 compared to other ALDH isozymes and dehydrogenases such as hALDH1B1, hALDH3A1, and hALDH2 (with IC50 values exceeding 57 μM).

Nitrefazole 是一种4-nitroimidazole 衍生物，对醛脱氢酶(ALDH)具有强烈而持久的抑制作用，醛脱氢酶是一种参与酒精代谢的酶。