aldh 1

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。

ALDH1A3-IN-2 是一种有效的 ALDH1A3 抑制剂，IC50 为 0.30 μM。ALDH1A3-IN-2 具有癌症疾病研究的潜力。

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。

ALDH1A2-IN-1 是一种活性位点导向的可逆 ALDH1A2 抑制剂，防止精子发生，可用于研究男性避孕化合物。

ALDH1A3-IN-1 (Compound 14) 是有效的 ALDH1A3抑制剂，可用于前列腺癌的研究， (IC50 = 0.63 μM; Ki = 0.46 μM)。

ALDH1A1-IN-3 是一种良好的、选择性的醛脱氢酶 1A1 (ALDH1A1) 抑制剂 (IC50: μM)。ALDH1A1-IN-3 可以有效的改善 HepG2 细胞的葡萄糖消耗。ALDH1A1-IN-3 能够用于进行改善糖代谢的研究。

ALDH1A1-IN-2 是一种有效的醛脱氢酶 1a1 (aldh1a1) 抑制剂，具有抗癌活性。ALDH1A1-IN-2 可用于研究乳腺癌、炎症或肥胖症。

NR6是一种新型、高效且高度选择性的ALDH1A3抑制剂。它能有效抑制间皮瘤多细胞球生长和中性粒细胞的招募。

ALDH2 modulator 1 是一种有效的且具有口服活性的乙醛脱氢酶-2 （ALDH2）调节剂。ALDH2 modulator 1 可使小鼠血液中的酒精含量降低。

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。

ALDH3A1-IN-2 (Compound 19) 作为一种高效的ALDH3A1抑制剂，其IC50值达到1.29 μM。由于醛脱氢酶 (ALDH) 在前列腺癌等多种肿瘤类型中的过表达，ALDH3A1-IN-2 显示出其在癌症疾病研究中的应用潜力。

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。

ALDH3A1-IN-1 是一种小分子 ALDH3A1 抑制剂，（IC50:1.61 μM)，可用于研究高脯氨酸血症和干燥-拉森综合征。

α-NETA 是一种高效的胆碱乙酰转移酶 (ChA) 抑制剂，也是一种 ALDH1A1 和趋化因子样受体 1 (CMKLR1) 拮抗剂,抗癌活性,抑制胆碱酯酶和乙酰胆碱酯 (AChE),剂量依赖性诱导 STZ 诱导的糖尿病小鼠体重和空腹血糖水平降低,显著降低肾损伤标志物的表达,可用于研究糖尿病肾病。

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.

MCI-INI-3 是一种选择性竞争性抑制剂，专门抑制人ALDH1A3 (Ki值为 0.55 μM，而对ALDH1A1的 Ki值为 78.2 μM)。MCIINI-3 能够抑制视黄酸的生物合成，并降低 GSC-83 和 GSC-326 胶质母细胞瘤细胞的活力。

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。

Aloenin (Aloenin A) A 是一种具有清除过氧自由基作用的天然产物，对 β-分泌酶 (BACE) 具有中等抑制活性。

Cyclosomatostatin TFA 作为一种有效的生长抑素(SST)受体拮抗剂，在直肠癌(CRC)细胞中通过抑制1型生长抑素受体(SSTR1)的信号传导，有效降低结细胞增殖、ALDH+细胞群体的大小以及球形成。

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]

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)

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。