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.
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-
(S)-Ceralasertib is a potent and selective inhibitor of sulfoximine morpholinopyrimidine ATR with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics. .
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.
DPNB-ABT 594 is a nitrobenzyl-caged ABT 594, a selective α4β2 nAChR agonist. One-photon uncaging evokes large inward currents and Ca2+transients on cell bodies and dendrites of medial habenular neurons in mouse brain slices. Two-photon uncaging induces fast nAChR-mediated currents. Photolyzed with high quantum yield of 0.20. Effective photolysis occurs using one- or two-photon excitation; one-photon uncaging requires illumination at 410 nm for 1.5-3 ms; two-photon uncaging requires illumination with appropriate two photon pulse laser at 710 nm for ~2 ms.
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
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%.