Aldehyde dehydrogenase 1 (ALDH1), which is a putative marker of breast cancer stem cells (CSCs), in triple negative breast cancer (TNBC) tissues.
Mitochondrial aldehyde dehydrogenase (ALDH2) is a member of the 19-strong human aldehyde dehydrogenase family of NADP+-dependent enzymes.
ALDH2, a mitochondrial enzyme responsible for metabolizing the major lipid peroxidation product, protects against acute ischemia/reperfusion injury and chronic heart failure. Activation of ALDH2, the main enzyme that catalyzes 4-HNE metabolism, is sufficient to protect the heart against acute ischemia-reperfusion injury.
ALDH2 is a key detoxifying enzyme. ALDH2 is most commonly associated with its role in ethanol metabolism, catalyzing the oxidation of ethanol-derived acetaldehyde to acetate.
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NCT-501 (NCT501) is a potent and highly selective inhibitor of ALDH1A1 with IC50 of 40 nM for hALDH1A1; exhibits high selectivity against ALDH1A1 over ALDH3A1, ALDH1B1, ALDH2 isozymes and other dehydrogenases such as HPGD and HSD17β4; excellent pharmacokinetics and in vitro ADME profiles.
WIN-18446 is a potent, covalent, orally active ALDH1A2 inhibitor with IC50 of 0.3 uM; potently inhibits spermatogenesis and causes infertility in vivo by inhibiting retinoic acid synthesis.
NCT-505 free base
NCT-505 free base (NCT505) is a potent, selective, orally available ALDH1A1 inhibitor with IC50 of 7 nM (hALDH1A1), exhibits high specificity over other ALDH isozymes and unrelated dehydrogenases; also exhibits IC50 of 30 nM in MIA PaCa-2 Aldefluor cell-based assays; demonstrates target engagement in CETSA asssay (EC50=3.4 uM), inhibits the formation of 3D spheroid cultures of OV-90 cancer cells, and potentiates the cytotoxicity of Paclitaxel in SKOV-3-TR, a Paclitaxel resistant ovarian cancer cell line.
ALDH1A inhibitor 673A
ALDH1A inhibitor 673A (ALDH1Ai 673A) is a potent, selective, pan-ALDH1A inhibitor with IC50 of 246, 230 and 348 nM for ALDH1A1, ALDH1A2 and ALDH1A3, respectively; shows no significant activity against ALDH2 (IC50 14 mM) or numerous other ALDH family members; ALDH1Ai 673A preferentially kills CD133+ ovarian cancer stem-like cells (CSCs), induces necroptotic CSC death, mediated, in part, by the induction of mitochondrial uncoupling proteins (UCPs) and reduction in oxidative phosphorylation; ALDH1Ai 673A is highly synergistic with chemotherapy, reducing tumor initiation capacity and increasing tumor eradication in vivo.
DKM 3-42 is a selective, covalent, in vivo-active ALDH3A1 inhibitor with IC50 of 50 uM against purified human ALDH3A1, targets ALDH3A1 catalytic cysteine, impairs both in situ and in vivo lung cancer pathogenicity; impairs A549 serum-survival in a dose-responsive manner, significantly attenuates tumor growth in vivo in A549 tumor xenografts in mice with dose of DKM 3-42 (50mg/kg ip) once per day.
ALDH3A1 inhibitor EN40
ALDH3A1 inhibitor EN40 is a potent and selective, covalent, in vivo-active inhibitor of ALDH3A1 with IC50 of 2 uM, demonstrates no activity against ALDH1A3 and ALDH6A1 at 30 uM; also does not show any observable competition against lysine-reactive probe labeling of A549 proteomes; specifically inhibits the lung cancer cell lines expressing ALDH3A1, but not in the cell lines that do not express ALDH3A1, inhibits ALDH3A1 activity and impairs lung cancer pathogenicity in vivo.
DIMATE is a novel irreversible, competitive, isoform-specific ALDH1 inhibitor, displays cytotoxic activity on human AML cell lines with IC50 of 1-15 uM; shows selective cytotoxicity in leukemic population enriched in LSCs, with no cytotoxicity for healthy hematopoietic stem cells; promotes the accumulation of apoptogenic aldehydes leading to apoptosis and tumor growth inhibition in xenograft mouse models.
CVT-10216 is a potent, highly selective, reversible inhibitor of ALDH2 with IC50 of 29 nM, shows no significant inhibition for ALDH1 (IC50=1,300 nM); demonstrates therapeutic potential to reduce excessive drinking and to suppress relapse in abstinent alcoholics; also shows both anxiolytic and antidipsotropic properties in rats; selectively suppresses binge eating of palatable food and attenuates dopamine release in the accumbens of sugar-bingeing rats.
Alda-1 is a small-molecule activator of ALDH2, particularly effective activator of ALDH2*2 (EC50= 20 uM; increases the activity of the mutant, ALDH2*2 (11-fold); causes slight inhibition of GTN denitration and did not increase GTN-induced sGC activation in the presence of either variant; no effect on ADH1.
NCT-505 (NCT505) is a potent, selective, orally available ALDH1A1 inhibitor with IC50 of 7 nM (hALDH1A1), exhibits high specificity over other ALDH isozymes and unrelated dehydrogenases; also exhibits IC50 of 30 nM in MIA PaCa-2 Aldefluor cell-based assays; demonstrates target engagement in CETSA asssay (EC50=3.4 uM), inhibits the formation of 3D spheroid cultures of OV-90 cancer cells, and potentiates the cytotoxicity of Paclitaxel in SKOV-3-TR, a Paclitaxel resistant ovarian cancer cell line.
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