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Lu AE98134 is a Selective Positive Modulator of NaV1.1 Channels

Edward Jenner 2021-01-30

Sodium channels are integral membrane proteins that form ion channels and conduct sodium ions (Na+) through the plasma membrane. These channels pass through three different states, which are resting state,…

Inflammation

LY-311727 is a Secretory non-Pancreatic Phospholipase A2 (sPLA2) Inhibitor

Edward Jenner 2021-01-28

Phospholipase A2 (PLA2s) is an enzyme that cleaves fatty acids in the second position of phospholipids. Specifically, PLA2s can specifically recognize the sn-2 acyl bond of phospholipids and catalyze the…

Osteoarthritis

CMC2.24 is an Orally Active Tricarbonylmethane Agent

Edward Jenner 2021-01-27

RAS is the name of a series of related proteins commonly expressed in all cell lineages and organs. Specifically, RAS is a prototype member of the Ras protein superfamily. All…

Peritonitis

Diflapolin is a Highly Active dual FLAP and sEH Inhibitor

Edward Jenner 2021-01-26

The arachidonic acid (AA) cascade plays a central role in the biosynthesis of lipid mediators (LMs) with anti-inflammatory properties cascade plays an important role in the biosynthesis of lipid mediators…

Cancer Immunology

SBP-7455 is an Orally Active Dual ULK1/ULK2 Autophagy Inhibitor

Edward Jenner 2021-01-22

Autophagy is a multi-step pathway initiated through the ULK preinitiation complex, which consists of unc-51-like autophagy activating kinase 1 (ULK1) or its homologue ULK2, autophagy-related protein 13 (ATG13), ATG101 and…

Inflammation

CRT0066854 is a Potent and Selective Atypical PKCs Inhibitor

Edward Jenner 2021-01-21

PKC isoenzymes are an important family of serine/threonine protein kinases. They contribute to many diverse cellular and tissue functions, as well as human disease pathologies including cancer development and progression.…

Cancer Immunotherapy

TAS6417 is a pan-Mutation Selective EGFR Inhibitor

Edward Jenner 2021-01-20

Despite dramatic response to first and second-generation EGFR TKIs, resistance emerges over time. The EGFR-T790M mutation accounts for more than half of drug resistance. Third generation (covalent mutation-specific: osimertinib) EGFR…

Cancer Immunotherapy

Neratinib is an Orally Available, Irreversible Tyrosine Kinase Inhibitor

Edward Jenner 2021-01-19

Neratinib is an irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively. Neratinib has inhibition of tyrosine kinase KDR and Src with…

Cancer Immunology

KMH-233 is a Reversible and Selective LAT1 Inhibitor

Edward Jenner 2021-01-18

Amino acids are essential for protein synthesis, they are supporting cell growth, and metabolism. System L belongs to the family of sodium-independent transport proteins. They can carry neutral amino acids…

Edward Jenner 2021-01-18

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You Missed

Pulmonary Arterial Hypertension (PAH)

PRX-08066 is an orally active 5-HT2BR Antagonist with Vasodilation Effect for PAH

Cancer Immune Metabolic Disease

Apocynin is a NADPH oxidase (NOX) Inhibitor for Metabolic and Inflammation Research

Uncategorized

Xylometazoline is an α-adrenergic Receptor Agonist for Nose Stuffiness Research

NASH obesity

Elafibranor is a PPARα/δ Agonist for Metabolic Disease Research

Immune System Research

Up to date immunology information

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