451lu

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

Lansoprazole sulfide (AG-177) is an active metabolite of Lansoprazole with similar activity.Lansoprazole is a proton pump inhibitor and antitubercular agent with an IC50= 0.59 µM against Mycobacterium tuberculosis.

Amphotericin X1 is a derivative of Amphotericin B with good antifungal activity. Amphotericin X1 inhibits Candida albicans 33/079, Cryptococcus neoformans 451, C.parapsilosis 937A, Aspergillus niger 57A and A.fumigatus (MICs: 1 μg/mL, 1 μg/mL, 8 μg/mL, 2

SKP-451 is an ATP-sensitive potassium (K+) channel agonist. It activates ATP-sensitive K+ channels, promoting the efflux of K+, leading to membrane hyperpolarization and inhibiting Ca2+ influx, which results in the relaxation of vascular smooth muscle. SKP-451 relaxes canine coronary arteries, rabbit basilar arteries, and vertebral arteries. Additionally, SKP-451 lowers mean arterial blood pressure in conscious spontaneously hypertensive rats (SHR). It holds potential for cardiovascular disease research.

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

LSPN451 is an effective xanthine oxidase inhibitor and may be used to treat hyperuricemia and gout.

Selective p300 histone acetyltransferase (HAT) inhibitor (IC50 = 50-500 nM). Exhibits approximately 100-fold selectivity for p300 over PCAF (IC50 = 200 μM). Inhibits p300-dependent transcription. Active in vivo. Lau et al (2000) HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol.Cell. 5 589 PMID:10882143 |Liu et al (2008) The structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature. 451 846 PMID:18273021 |Burns et al (2005) Iso-coenzyme A. J.Biol.Chem. 280 16550 PMID:15708855 |Cebrat et al (2003) Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg.Med.Chem. 11 3307 PMID:12837541

Ki-20227 is a specific c-Fms tyrosine kinase(CSF1R) inhibitor (IC50: 2 nM). It also has certain inhibitory against VEGFR2(IC50: 12 nM) and c-Kit/PDGFRβ(IC50: 451/217 nM), respectively.

This compound is a dual 5-HT1A/5-HT7 receptor antagonist (5-HT1A Ki = 8 nM, Kb = 0.04 nM; 5-HT7 Ki = 451 nM, Kb = 460 nM) with additional inhibitory activity against PDE4B/PDE7A (PDE4B IC50 = 80.4 μM; PDE7A IC50 = 151.3 μM). Its antidepressant-like effect surpasses that of the reference agent, escitalopram.

Compound 22, a 5-hydroxynitrile rubber 7 receptor antagonist (5-HT1A Ki=8 nm, Kb=0.04 nm; 5-nitrile rubber 7K I=451 nm, Kb=460 nm), exhibits inhibitory activity against PDE4B/PDE7A (PDE4B IC50=80.4 μM; PDE7A IC50=151.3 μM). It demonstrates significant passive biofilm penetration capabilities and high metabolic stability in vitro. Pharmacological assessment has revealed precognitive and antidepressant effects in rat behavioral tests, highlighting its potential therapeutic applications.

2-Fluorocinnamic acid is a useful organic compound for research related to life sciences. The catalog number is T64995 and the CAS number is 451-69-4.

EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA/kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimental disease models, and on its low side effect potential.

EGFR-IN-451 is an EGFR inhibitor, attenuating Ang II-induced Kidney Fibrosis.

α-Glucosidase-IN-24 (Compound 13), an α-Glucosidase inhibitor derived from Swertia kouitchensis [1], exhibits an IC50 value of 451 μM.

Rocatinlimab (AMG 451) (KHK4083) is a fully human, non-fucosylated IgG1 anti-OX40 monoclonal antibody indicated for atopic dermatitis (AD) research [1].

Pebezertinib (BLU 451) is an orally effective inhibitor of EGFR, capable of penetrating the central nervous system (CNS). It is utilized in research targeting non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertions.

Azerutamig is a dual-specificity antibody targeting KLRK1/ERBB2 of type (H-γ1_L-κ)_scFvkh-H-γ1(h-CH2-CH3).