CHI3L1-IN-3 

CHI3L1-IN-3 is a CHI3L1 inhibitor. CHI3L1-IN-3 binds to CHI3L1 with K_ds of 13.76 μM and 13.5 μM in MST and SPR assays, respectively. CHI3L1-IN-3 demonstrates extended plasma half-lives and microsomal stability, along with reduced intrinsic clearance. CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass and inhibits migration in a 3D multicellular glioblastoma (GBM) spheroid model. CHI3L1-IN-3 can be used for the study of GBM^[1].

CHI3L1-IN-3 (Compound 11g) exhibits enhanced stability, with increased plasma half-lives of 2.0 h (mouse) and 2.5 h (human), and microsomal half-lives of 2.2 h (mouse) and 2.8 h (human) and lower clearance rates of 15 mL/min/mg (mouse) and 19 mL/min/mg (human)^[1].
CHI3L1-IN-3 (50 μM, 72 h) demonstrates low cytotoxicity in hBMECs and HepG2 cells and no cytotoxicity in NHA cells^[1].
CHI3L1-IN-3 (5-25 μM, 72 h) shows a dose-dependent reduction in cell viability of GBM spheroids^[1].
CHI3L1-IN-3 (10 μM, 72 h) reduces spheroid weight by over 50 %, consistent with widespread cell death and loss of structural cohesion^[1].
CHI3L1-IN-3 (10 μM, 24-96 h) suppresses GBM spheroids migration by 60 %^[1].
CHI3L1-IN-3 exhibits antiproliferative activity in glioblastoma cell lines, with IC₅₀ values of 2.19 μM in U251 MG and 5.06 μM in T98G cells^[1].
CHI3L1-IN-3 (5-25 μM, 72 h) reduces pSTAT3 levels dose-dependently in GBM spheroids^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

563.66

C₃₀H₃₃N₃O₆S

COC(C(OC)=C1)=CC(C2=O)=C1N=C(SCC(NC3=CC=C(CC)C=C3)=O)N2CCC4=CC=C(OC)C(OC)=C4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kaur B, et al. Lead optimization of a CHI3L1 inhibitor for Glioblastoma: Enhanced target engagement, pharmacokinetics, and efficacy in 3D spheroid models. Eur J Med Chem. 2025 Jun 28;297:117924.  [Content Brief]