| Name | Lanraplenib |
| Description | Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) being developed for treating inflammatory diseases. It inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. |
| In vitro | Lanraplenib (GS-9876) inhibits glycoprotein VI (GPVI)-induced phosphorylation of linker for activation of T cells and phospholipase Cγ2, platelet activation and aggregation in human whole blood, and platelet binding to collagen under arterial flow [2]. Lanraplenib inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells (EC50s: 24-51 nM). Lanraplenib inhibits anti-IgM mediated CD69 and CD86 expression on B-cells (EC50: 112±10 nM and 164±15 nM, respectively) and anti-IgM /anti-CD40 co-stimulated B cell proliferation (EC50: 108±55 nM). In human macrophages, Lanraplenib inhibits IC-stimulated TNFα and IL-1β release (EC50: 121±77 nM and 9±17 nM, respectively) [1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.51 mM), Sonication is recommended.
DMSO : 24.2 mg/mL (54.57 mM), Sonication is recommended.
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| Keywords | Syk | Spleen tyrosine kinase | Lanraplenib | Inhibitor | inhibit | GS9876 | GS 9876 |
| Inhibitors Related | URMC-099 | Fostamatinib | Entospletinib | Ellagic acid | TC-S 7003 | Piceatannol | Cerdulatinib | ANTHRAQUINONE-2-CARBOXYLIC ACID | GSK1904529A | R406 | Gusacitinib | Cerdulatinib hydrochloride |
| Related Compound Libraries | Highly Selective Inhibitor Library | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | Angiogenesis related Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |
United States
