RANKL-IN-1

RANKL-IN-1 is a selective and orally active Receptor Activator of Nuclear Factor-κ B Ligand (RANKL) inhibitor with a KD value of 7.6 μM. RANKL-IN-1 exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC50 value of 0.07 μM and SI of 82.57. RANKL-IN-1binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 can be used for the research of metabolic disease, such as osteoporosis[1].

Product Specifications

UNSPSC

12352005

Target

ERK; JNK; MMP; NF-κB; p38 MAPK; RANKL/RANK ; Reactive Oxygen Species (ROS)

Related Pathways

Immunology/Inflammation; MAPK/ERK Pathway; Metabolic Enzyme/Protease; NF-κB; Stem Cell/Wnt

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Smiles

CC1=C(C2=CC3=NC=CN=C31)C=C[C@@]4(C2=CC[C@@]5([C@@]4(CC[C@@]6([C@H]5C[C@](C(N7CCC(CC7)N8CCNCC8)=O)(CC6)C)C)C)C)C

Molecular Formula

C40H55N5O

Molecular Weight

621.90

References & Citations

[1]Fu X, et al. Design, Synthesis, and Biological Evaluation of Heterocycle-Fused Celastrol Derivatives as Potent Antiosteoporosis Agents by Blocking RANKL-Induced Activation of the NF-κB and MAPK Signaling Pathways. J Med Chem. 2025 Aug 28;68 (16) :17678-17704.