aldh 1

ALDH1A3-IN-3 (compound 16), a powerful ALDH1A3 inhibitor with an IC50 of 0.26 μM, serves as an effective ALDH3A1 substrate. It is utilized in prostate cancer research.

ALDH2 modulator 1 is a potent, orally active modulator of acetaldehyde dehydrogenase-2 (ALDH2), which reduces blood alcohol levels in mice.

ALDH1A3-IN-2 is a potent ALDH1A3 inhibitor with an IC50 of 0.30 μM.ALDH1A3-IN-2 has potential for cancer disease research.

ALDH3A1-IN-2 (Compound 19), a potent inhibitor of aldehyde dehydrogenases (ALDHs), demonstrates high efficacy against ALDH3A1 with an IC50 of 1.29 μM. Given the overexpression of ALDHs in multiple tumor types, including prostate cancer, ALDH3A1-IN-2 holds significant potential for cancer research [1].

ALDH1A1-IN-4 (compound A1) functions as a powerful inhibitor of aldehyde dehydrogenase (ALDH) A1, exhibiting an IC 50 value of 0.32 μM. This compound is significant in cancer research [1].

ALDH1A2-IN-1 is a reversible inhibitor of the active site of ALDH1A2, showing a significant affinity for the enzyme with an IC50 value of 0.91 μM and a Kd value of 0.26 μM. This compound interacts hydrophobically with the enzyme, contributing to its inhibitory properties.

ALDH1A3-IN-1 (Compound 14) is a potent inhibitor of ALDH1A3, with IC50 = 0.63 μM and Ki = 0.46 μM, and is utilized in prostate cancer research [1].

ALDH1A1-IN-3 is a good and selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1) (IC50: μM).ALDH1A1-IN-3 is effective in improving glucose consumption in HepG2 cells.ALDH1A1-IN-3 can be used for studies to improve glucose metabolism.

ALDH1A1-IN-2 is a potent aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitor with anticancer activity and may be used in research on breast cancer, inflammation, or obesity.

ALDH3A1-IN-1 (Compound 18) is a potent ALDH3A1 inhibitor with an IC 50 of 1.61 μM. It is more effective than DEAB against patient-derived primary prostate tumor epithelial cells, both as a single agent and in combination with docetaxel [1].

1. Aloenin (Aloenin A) and aloe-emodin are active principles for inhibition of c-ADH and c-ALDH activities in vitro.

MeDTC (S-Methyl-N,N-diethylthiocarbamate Sulfone), a metabolite of Disulfiram, serves as a potent and irreversible inhibitor of aldehyde dehydrogenase (ALDH) [1].

Cyclosomatostatin TFA, a potent somatostatin (SST) receptor antagonist, inhibits type 1 somatostatin receptor (SSTR1) signaling, reducing cell proliferation, the size of the ALDH+ cell population, and sphere-formation in colorectal cancer (CRC) cells [1].

Aldehyde dehydrogenase NAD(P) (ALDH) is an enzyme that facilitates the conversion of aldehydes into their respective carboxylic acids while simultaneously reducing the cofactor NAD(P) to NAD(P)H, making it a key component in biochemical research. This enzyme plays a crucial role in mitigating aldehyde stress by being part of the body's array of enzymatic defenses [1].

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)

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 is a Potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50: 29 nM). CVT-10216 also has inhibitory effect of ALDH-1 (IC50: 1.3 μM). CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.

Alda-1 is an ALDH2 agonist, a cell-permeable activator of both the wild-type ALDH2*1 and the Asian E487K mutant ALDH2*2 forms of mitochondrial aldehyde dehydrogenase 2 (mtALDH2).

1. Raspberry ketone (p-Hydroxybenzyl acetone) is cytotoxic to melanocytes through the binding of RK-derived quinones to thiol proteins and the pro-oxidant activity of the RK-oligomer, the exposure of human skin to RK can cause chemical occupational leukoderma. 2. Raspberry ketone is marketed on the Internet as a food supplement.

Cyclosomatostatin Acetate is an effective antagonist of the somatostatin receptor.Cyclosomatostatin Acetate inhibits SSTR1 signaling and decreases cell proliferation, ALDH+ cell population size, and sphere-formation in colorectal cancer cells.