a-272

Rutamycin is a macrolide antibiotic of the oligomycin group obtained from Streptomyces rutgersensis. It inhibits various ATPases and uncouples oxidative phosphorylation from electron transport.

ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 is a potent and orally active KCNQ2/Q3 potassium channel opener (EC50: 0.38 μM). ICA-27243 also has antiepileptic and anticonvulsant effects.

KGA-2727 is a potent and selective SGLT1 inhibitor, with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 for the treatment of diabete.

Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.

AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A/-B/-C with Kd values ranging from 23-289 nM.

GNE-272 is a potent and highly selective inhibitor of the CBP/EP300 bromodomains. This product inhibits CBP and EP300 with IC50 values of 0.02 μM and 0.03 μM, respectively, exhibiting 650-fold selectivity over BRD4 (IC50 = 13 μM). In cell-based assays, it effectively inhibits MYC expression (EC50 = 0.91 μM) without significant off-target activity against various kinases, receptors, or cytochrome P450 isoforms. As a selective in vivo probe, GNE-272 serves as a vital pharmacological tool for studying CBP/EP300 functions in acute myeloid leukemia (AML) and other cancers.

Imarikiren (also known as TAK-272) is a potent, highly selective, orally bioavailable direct renin inhibitor primarily used for treating diabetic nephropathy. In hPRA assays, TAK-272 exhibits strong inhibitory activity against human renin (IC50 = 2.1 nM) and demonstrates excellent selectivity over other aspartic proteases such as pepsin (IC50 > 10 μM) and cathepsin D (IC50 > 10 μM). In rats, TAK-272 shows significantly improved pharmacokinetic properties (F = 25.2%) and, upon oral administration (3 and 10 mg/kg), exhibits a dose-dependent, potent, and sustained antihypertensive effect. Currently, TAK-272 HCl is undergoing human clinical trials.

Antibacterialagent 272 (Compound Z22) is a potential antibacterial agent that targets the DNA and DNA-topoisomerase II (DNA-Topo II) complex. It exhibits strong antibacterial activity, with a minimum inhibitory concentration (MIC) of 1 μg/mL against Staphylococcus aureus 25923 and 29213, 2 μg/mL against Staphylococcus epidermidis 12228, 2-4 μg/mL against Enterococcus faecalis, and 4 μg/mL against Pseudomonas aeruginosa 9027 and 27853. Antibacterialagent 272 binds by intercalating between DNA base pairs, disrupting the normal function of bacterial DNA, and is suitable for research into bacterial infectious diseases.

Anticanceragent 272 (Compound 2) is an anticancer agent demonstrating significant activity against bladder cancer cells (T-24) with an IC50 of 2.81 μM. It depletes glutathione (GSH) through a Fenton-like reaction, generating reactive oxygen species (ROS) and hydroxyl radicals (•OH), thereby inducing apoptosis and ferroptosis. Anticanceragent 272 enhances chemodynamic therapy (CDT) and promotes tumor cell death through mitochondrial dysfunction and autophagy. It holds potential for further research in bladder cancer.

Kynostatin-272 is a HIV protease inhibitor. KNI-272 blocked the maturation of viral particles.

AL-272 is a bio-active chemical.

Janthitrem A is a mycotoxin that has been found inP. janthinellum.1It induces tremors in mice and decreases the time to fall from the rotarod when administered at a dose of 4 mg/kg.2Janthitrem A (20 μg/g) also reducesW. cervinatalarvae weight gain and food consumption. 1.Gallagher, R.T., Latch, G.C., and Keogh, R.G.The janthitrems: Fluorescent tremorgenic toxins produced by Penicillium janthinellum isolates from ryegrass pasturesAppl. Environ. Microbiol.39(1)272-273(1980) 2.Babu, J.V., Popay, A.J., Miles, C.O., et al.Identification and structure elucidation of janthitrems A and D from Penicillium janthinellum and determination of the tremorgenic and anti-insect activity of janthitrems A and BJ. Agric. Food Chem.66(50)13116-13125(2018)

Ac-VEID-AMC is a fluorogenic substrate based on the caspase-6 cleavage site in lamin A at amino acids VEID during apoptosis.1It has also been reported to be cleaved by related proteases, including caspase-8.2Caspase activity can be quantified by fluorescent detection of free AMC (also known as 7-amino-4-methylcoumarin), which is excited at 340-360 nm and emits at 440-460 nm. 1.Talanian, R.V., Quinlan, C., Trautz, S., et al.Substrate specificities of caspase family proteasesJ. Biol. Chem.272(15)9677-9682(1997) 2.Chae, H.J., Park, K.M., Lee, G.Y., et al.Je-Chun-Jun induced apoptosis of human cervical carcinoma HeLa cellsActa Pharmacologica Sinica25(10)1372-1379(2004)

Negative control for st-Ht31 . Gorshkov et al (2017) AKAP-mediated feedback control of cAMP gradients in developing hippocampal neurons. Nat.Chem.Biol. 13 425 PMID:28192412 |Vijayaraghavan et al (1997) Protein kinase A-anchoring inhibitor peptides arrest mammalian sperm motility. J.Biol.Chem. 272 4747 PMID:9030527 |Vincent et al (2017) Signaling: Spatial regulation of axonal cAMP. Nat.Chem.Biol. 13 348 PMID:28328917

Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 |1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of acyl-CoA: Cholesterol acyltransferase produced by Penicillium griseofulvum F1959. J. Antibiot. (Tokyo) 55(11), 1004-1008 (2002).|2. Lee, S.W., Rho, M.C., Choi, J.H., et al. Inhibition of diacylglycerol acyltransferase by phenylpyropenes produced by Penicillium griseofulvum F1959. J. Microbiol. Biotechnol. 18(11), 1785-1788 (2008).|3. Horikoshi, R., Goto, K., Mitomi, M., et al. Identification of pyripyropene A as a promising insecticidal compound in a microbial metabolite screening. J. Antibiot. (Tokyo) 70(3), 272-276 (2017).

CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.

Neratinib-D6 (Standard) is a reference standard of Neratinib-D6 intended for quantitative analysis, quality control, and related biochemical research applications. Neratinib-d6 is the deuterated form of Neratinib. Neratinib (HKI-272) is an orally active, irreversible tyrosine kinase inhibitor that suppresses the activity of HER2 and EGFR, with IC50 values of 59 nM and 92 nM, respectively.