- PluriSIn #1 (NSC 14613)
- Gimeracil
- Mycophenolate Mofetil
- Trilostane
- AGI-5198
- CPI-613
| Alda 1ALDH2 activator |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.96%
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- HPLC
- NMR (Nuclear Magnetic Resonance)
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- Datasheet
Chemical structure
| Kinase experiment [1]: | |
Kinase assays | Dehydrogenase activity was measured as conversion of NAD (1 mM) to NADH in the presence of formaldehyde, acetaldehyde, or propionaldehyde (1 mM each) by monitoring the change in absorbance at 340 nm at 25 °C. The reactions were performed in 50 mM sodium pyrophosphate buffer (pH 9.0) containing 10 mM MgCl2 and 10 μM Alda-1 or 0.5% (v/v) DMSO as a vehicle control. |
| Animal experiment [2]: | |
Animal models | Mouse xenograft SCC VII tumor model |
Dosage form | Alda-1 (3 mM in 95% ethanol solution in a volume of 0.25 ml) was applied locally on the skin. |
Application | Concomitant topical application of the ALDH2 activator, Alda-1, effectively reduced the severity and delayed the onset of radiation-induced dermatitis in mice. Therefore, Alda-1, may be used as an adjunct to radiation therapy for the treatment of solid tumors in which radiation-induced dermatitis is an important clinical problem. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Beretta M, Gorren AC, Wenzl MV, Weis R, Russwurm M, Koesling D, Schmidt K, Mayer B. Characterization of the East Asian variant of aldehyde dehydrogenase-2: bioactivation of nitroglycerin and effects of Alda-1. J Biol Chem. 2010 Jan 8;285(2):943-52. [2] Ning S, Budas GR, Churchill EN, Chen CH, Knox SJ, Mochly-Rosen D. Mitigation of radiation-induced dermatitis by activation of aldehyde dehydrogenase 2 using topical alda-1 in mice. Radiat Res. 2012 Jul;178(1):69-74. | |
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| Cas No. | 349438-38-6 | SDF | Download SDF |
| Chemical Name | N-(benzo[d][1,3]dioxol-5-ylmethyl)-2,6-dichlorobenzamide | ||
| Canonical SMILES | ClC1=CC=CC(Cl)=C1C(NCC2=CC=C3OCOC3=C2)=O | ||
| Formula | C15H11Cl2NO3 | M.Wt | 324.16 |
| Solubility | ≥15.15mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: N/A
Alda 1 is an activator of aldehyde dehydrogenase 2 (ALDH2).
Alda 1 increases activity of wild-type ALDH2*1 and variant ALDH2*2 (by ~2-fold and 11-fold respectively), Capable of partly restoring mutant ALDH2*2 activity, and protective against cardiac ischemia.
In vitro: In the present study , Alda-1 increased acetaldehyde oxidation by ALDH2*1 and ALDH2*2 approximately 1.5- and 6-fold, respectively, regarding GTN bioactivation and the effects of Alda-1. To similar extent, Alda-1 induced the esterase activities of both enzymes as the coenzyme NAD. NAD pronounced inhibition occurring at > 5mM, its the effect was biphasic. In the presence of 1 mM NAD, Alda-1 induced ALDH2*2-catalyzed ester hydrolysis 73-fold, whereas the NAD-induced activity of ALDH2*1 was inhibited on account of 20-fold increased inhibitory potency of NAD in the presence of the drug. ALDH2*2 displayed 7-fold lower GTN denitrating activity and GTN affinity than ALDH2*1, but the rate of nitric oxide formation was only reduced 2-fold. Soluble guanylate cyclase (sGC) activation was more pronounced than with wild type ALDH2 at saturating GTN. Alda-1 caused slight inhibition of GTN denitration, and in the presence of either variant, GTN-induced sGC activation was increased. The present results imply that established ALDH2 activities stimulated by Alda-1, which improved NAD binding but does not improve the GTN binding affinity of the Asian variant. In addition, an unexpected discrepancy between GTN reductase activity and sGC activation was revealed, which suggested that GTN denitration and bioactivation may display independent pathways of ALDH2-catalyzed GTN biotransformation [1].
In vivo: Alda-1 (a high-throughput screen yielded a small-molecule activator of ALDH2, administered to rats before an ischemic event) reduced infarct size by 60%, most likely through the inhibition ofthe formation of cytotoxic aldehydes. Thus, pharmacologic enhancement of ALDH2 activity may be benefit to patients with wild-type or mutant ALDH2 who are subjected to cardiac ischemia, such as during coronary bypass surgery [2].
Clinical trial: Clinical study has been conducted.
References:[1]. Beretta M, Gorren AC, Wenzl MV, Weis R, Russwurm M, Koesling D, Schmidt K, Mayer B. Characterization of the East Asian variant of aldehyde dehydrogenase-2: bioactivation of nitroglycerin and effects of Alda-1. J Biol Chem. 2010 Jan 8;285(2):943-52. [2]. Chen CH, Budas GR, Churchill EN, Disatnik MH, Hurley TD, Mochly-Rosen D. Activation of aldehyde dehydrogenase-2 reduces ischemic damage to the heart. Science. 2008 Sep 12;321(5895):1493-5.
