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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.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
GY02847 |
NCT-501 |
1802088-50-1 | 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. |
GY06958 |
WIN-18446 |
1477-57-2 | 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. |
GY10366 |
NCT-505 free base |
2231079-74-4 | 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. |
GY10545 |
ALDH1A inhibitor 673A |
109437-62-9 | 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. |
GY05244 |
DKM 3-42 |
164925-73-9 | 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. |
GY05198 |
ALDH3A1 inhibitor EN40 |
2094547-67-6 | 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. |
GY05161 |
DIMATE |
350229-29-7 | 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. |
GY04320 |
CVT-10216 |
1005334-57-5 | 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. |
GY03193 |
Alda-1 |
349438-38-6 | 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. |
GY05591 |
NCT-505 |
2231079-75-5 | 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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