Cellular Metabolism

AUTOPHAGY

Ion & Other Channels

Epigenetics

Cytoskeleton

Kinases

Mitochondria

Nuclear Receptors

Bioactive Lipids

Ubiquitin Proteasome

Biochemical Targets

Biological systems function through the complex interplay of a multitude of enzymes, transporters, ion channels, receptors, and other reactive molecules. The actions of these effectors can be modified by endogenous ligands, externally applied chemical reagents, or genetic or epigenetic changes to relevant genes. Pathological states can result when the actions of any of these biological effectors are perturbed.

Featured Products:

Herboxidiene | Spliceosome inhibitor

Herboxidiene (142861-00-5) is a novel polyketide fermentation product produced by Streptomyces chromofuscus, originally discovered by screening for herbicidal activity. Potent and selective inhibitor of spliceosome subunit SF3b.2 Specifically targets SAP155, a subunit of SF3b responsible for pre-mRNA splicing.3 Displays anti-angiogenic activity via down-regulation of VEGFR-2 and HIF-1α.4 Spliceosome inhibitors have attracted enormous attention due to their potential use in cancer treatment.5

YM-254890 | Gq inhibitor

YM-254890 (568580-02-9) is a novel Gαq/11 inhibitor.1 U46619-induced platelet aggregation is inhibited but phorbol ester- or ionophore-induced aggregation is not2 (IC50 = 0.1-0.2 μM)1. It blocks Pasteurella multocida toxin-mediated activation of Gαq.3 A highly useful new tool for studying Gαq/11-coupled receptor signaling and resulting cellular events.4

7-Cl-O-Nec1 | RIP1 inhibitor

7-Cl-O-Nec1 (852391-15-2) is a necrostatin-1 (Cat.# 10-1162) analogue with superior potency (IC50 = 206nM vs 494nM), selectivity and metabolic stability in blocking RIP1.1,2 7-Cl-O-Nec1 shows no off-target inhibition of indolamine-2,3-deoxygenase (IDO) in contrast to Necrostatin-1 (Nec-1).3,4 7-Cl-O-Nec1 showed higher activity in inhibiting necroptosis in Jurkat cells than Necrostatin-1 (EC50 = 210 nM vs. EC50 = 490 nM), no non-specific cytotoxicity at high concentrations (100 μM) and reasonable pharmacokinetic characteristics when used in mice.2 7-Cl-O-Nec1 is recommended for cellular and in vivo use over Necrostatin-1.5

New Products

BIOCHEMICAL TARGETS

Processes and Diseases

CUSTOM SYNTHESIS

CHEMICAL LIBRARIES

FOCUS NEWS:

Update on the Latest Anti-SARS-CoV-2 Molecules

The emergence of SARS-CoV-2 has precipitated an unprecedented effort by the scientific community to find and develop potential therapeutics and vaccines for this new virus to halt the ongoing pandemic’s onslaught. Fortunately, the SARS-CoV-2 genome is highly...

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