(S)-Ceralasertib is a potent and selective inhibitor of sulfoximine morpholinopyrimidine ATR with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics. .
Ceralasertib is an orally available inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase. Ceralasertib selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine threonine protein kinase CHK1. This prevents ATR-
Volasertib (BI 6727) trihydrochloride is a dihydropteridinone derivative that exhibits potent and selective inhibition of Polo-like kinase 1 (PLK1), PLK2, and PLK3. It acts as an orally active ATP-competitive inhibitor with an IC50 of 0.87 nM against PLK1. Additionally, Volasertib trihydrochloride demonstrates IC50 values of 5 nM and 56 nM against PLK2 and PLK3, respectively. Its mechanism of action includes inducing mitotic arrest and apoptosis. Furthermore, Volasertib trihydrochloride has been shown to possess significant antitumor activity in various cancer models.
N-Formyl-Met-Ala-Ser is a peptide that binds to formyl peptide receptors on neutrophils. This N-Formylmethionine-containing peptide, known as fMet-Ala-Ser, is among the most potent and well-known peptides that interact with these receptors.
Porfimer sodium is t he sodium salt of a mixture of oligomers formed by ether and ester linkages of up to eight porphyrin units with photodynamic activity. Absorbed selectively by tumor cells, porfimer produces oxygen radicals after activation by 630 nm w
(±)11(12)-EET is a fully racemic version of the R S enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes.[1][2][3[]A higher proportion of 11(R),12(S)-EET is produced by the CYP450 isoforms CYP2C23 and CYP2C24 while CYP2B2 produces a higher proportion of 11(S),12(R)-EET.[3]11(12)-EET has been shown, along with 8(9)-EET to play a role in the recovery of depleted calcium pools in cultured smooth muscle cells[4] It also inhibits basolateral 18-pS potassium channels in the renal cortical collecting duct when used at a concentration of 100 nM.[5]11(12)-EET (50 μg kg per day) increases adhesion of isolated peripheral blood leukocytes in a chamber coated with P-selectin and ICAM-1 but does not affect choroidal neovascularization size following laser photocoagulation[6] It also has anti-inflammatory, angiogenic, and cardioprotective properties[7]
Green fluorescent taxol derivative. Used for microtubule imaging. Binds microtubules with high affinity (Ka ~ 107M-1). Excitation/emission maximum λ ~ 496/526 nm. Lillo et al (2002) Location and properties of the Tax. binding center in microtubules: a picosecond laser study with fluorescent taxoids. Biochemistry. 41 12436 PMID:12369834 |Diaz et al (2000) Molecular recognition of Tax. by microtubules. Kinetics and thermodynamics of binding of fluorescent Tax. derivatives to an exposed site. J.Biol.Chem. 275 26265 PMID:10818101
Bimatoprost grenod(15-(6-nitroxyhexanoyl)-17-phenyl trinor PGF2α) is a nitric oxide-donating derivative of 17-phenyl trinor PGF2α.1It increases cGMP levels in rabbit aqueous humor and iris ciliary body when topically administered at a concentration of 0.042%. Topical administration of 15-(6-nitroxylhexanoyl)-17-phenyl trinor PGF2α(0.14%) reduces intraocular hypertension (IOP) in a rabbit model of hypertonic saline-induced transient ocular pressure. It also reduces IOP in a cynomolgus monkey model of laser-induced ocular hypertension when administered topically at a concentration of 0.042%.