c-Fms Inhibitor

c-Fms-IN-13 (compound 14) is a potent FMS kinase inhibitor with an IC₅₀ value of 17 nM. c-Fms-IN-13 can be used as an anti-inflammatory agent.

GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.

BRD4-BD1/2-IN-3 (Compound B6) is a selective BRD4 BD2 inhibitor with an IC₅₀ of 0.41  nM for BRD4 BD2 over BRD4 BD1. BRD4-BD1/2-IN-3 significantly inhibits the LPS (HY-D1056)-induced expression of IL-6. BRD4-BD1/2-IN-3 shows anti-inflammatory activities by modulating the TNF and NF-κB signaling pathway. BRD4-BD1/2-IN-3 can be used for inflammatory diseases research.

AMG-820 is a fully human IgG2 antibody that targets CSF-1R. AMG-820 inhibits binding of the ligands CSF1 and IL34 and subsequent ligand-induced receptor activation. The isotype control for AMG-820 can refer to Human IgG2 kappa, Isotype Control (HY-P99002).

JNJ-28312141 is an inhibitor for colony-stimulating factor-1 receptor (CSF-1R or FMS), with an IC₅₀ of 0.69 nM. JNJ-28312141 inhibits proliferation of BDBM, MV-4-11, M-o7e, TF-1 with an IC₅₀s of 2.6, 21, 41 and 150 nM, respectively. JNJ-28312141 exhibits anti-inflammatory activity in mouse arthritis model.

Segigratinib is a fibroblast growth factor receptor tyrosine kinase inhibitor, with antineoplastic effect.

JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC₅₀ values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity.

Sotuletinib (BLZ945) dihydrochloride is a potent, selective, orally active and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC₅₀ of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs. Sotuletinib dihydrochloride can be used for microglia depletion, and for tumor and CNS-related disease research.

Axl/Mer/CSF1R-IN-2 (Comp 4) is a Axl, Mer and CSF1R inhibitor.

IACS-9439 is a potent, selective, and orally active CSF1R inhibitor with a K_i value of 1 nM inhibitor. IACS-9439 can be used for advanced solid tumors research.

ABD-295, a biphenylsulfide derivative, is an antiresorptive agent, osteoclast inhibitor. ABD-295 has potent inhibitory effects on osteoclastic bone resorption in vitro. ABD-295 prevents ovariectomy-induced bone loss in vivo^[1].

CSF1R-IN-5 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-5 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-5 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 11).

CSF1R-IN-7 (Formula I) is a CSF-1R inhibitor. CSF1R-IN-7 can be used for Alzheimer’s disease research.

CSF1R-IN-9 (Compound 46) is a CSF-1R inhibitor with an IC₅₀ of 0.028 μM.

CSF1R-IN-23 (Compound 7dri) is a selective inhibitor for colony-stimulating factor-1 receptor (CSF1R), with IC₅₀ of 36.1 nM. CSF1R-IN-23 serves as antineuroinflammatory agent in mouse model. CSF1R-IN-23 is blood brain barrier (BBB) permeable.

Ataquimast is a COX-2 inhibitor that inhibits the release of leukotrienes, TNF-α and GM-CSF. Ataquimast can be used in the study of advanced receptor-positive breast cancer.

c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis.

CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC₅₀ of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22%.

CSF1R/c-Kit-IN-2 is a dual CSF-1R/c-Kit inhibitor with a c-Kit-biased profile, exhibiting inhibitory activity against CSF-1R (IC₅₀ = 6.84 nM), c-Kit (IC₅₀ = 0.95 nM), FYN (IC₅₀ = 11.4 nM), ABL1 (IC₅₀ = 14.2 nM), and CSK (IC₅₀ = 118 nM). CSF1R/c-Kit-IN-2 can be used for the research of neuroinflammation-associated neurodegenerative diseases.

cFMS Receptor Inhibitor IV (Compound 42) is a potent cFMS inhibitor with an IC₅₀ of 0.017 μM.