2. Neuronal Signaling Immunology/Inflammation
  3. Amyloid-β CD47
  4. CL121

CL121 is a Glutaminyl Cyclase inhibitor with an IC50 of 0.07 μM against human sQC and an IC50 of 0.54 μM against human gQC. CL121 reduces the level of pyroglutamate (pE)-modified CD47 on the surface of cancer cells. CL121 exhibits anti-tumor activity against triple-negative breast cancer.

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CL121

CL121 Chemical Structure

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Description

CL121 is a Glutaminyl Cyclase inhibitor with an IC50 of 0.07 μM against human sQC and an IC50 of 0.54 μM against human gQC. CL121 reduces the level of pyroglutamate (pE)-modified CD47 on the surface of cancer cells. CL121 exhibits anti-tumor activity against triple-negative breast cancer[1].

In Vitro

CL121 potently inhibits purified human sQC with an IC50 of 0.07 μM and human gQC with an IC50 of 0.54 μM[1].
CL121 (10-40 μM; 72 h) reduces surface pE-CD47 modification in a dose-dependent manner on MDA-MB-231 cells without affecting total CD47 expression[1].
CL121 (10-40 μM) enhances macrophage-mediated phagocytosis of KYSE30 cells, with the most potent effect at 20 μM, while higher concentrations (40 μM) show reduced activity[1].

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

CL121 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-231, KYSE30, MCF-10A, Het1A
Concentration: 50 μM
Incubation Time: 72 h
Result: Resulted in cell viability above 75% across all tested cell lines.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 CLz/F Vz/F AUC0-∞
Rat[1] 10 mg/kg i.p. 4976 ± 889 μg/L 0.25 h 2.48 ± 2.15 h 1.9 ± 0.4 L/h/kg 6 ± 3.84 L/kg 5431 ± 1253 μg/L·h
In Vivo

CL121 (10-20 mg/kg; i.p.; once daily; for 3 consecutive weeks) exhibits significant anti-tumor activity in a mouse MDA-MB-231 xenograft model[1].

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

Animal Model: BALB/c nude (female)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; daily; 3 weeks
Result: Reduced average tumor volume to 154 mm3 (from 227 mm3 in controls) and average tumor weight to 129.05 mg (from 191.49 mg in controls) at 10 mg/kg, with statistically significant tumor weight reduction (P < 0.01).
Reduced average tumor volume to 195 mm3 and average tumor weight to 173.69 mg at 20 mg/kg, with no statistically significant difference compared to controls.
Significantly reduced intratumoral pE-CD47 expression relative to controls at both doses, with 10 mg/kg showing statistically significant reduction (P < 0.05) and 20 mg/kg showing stronger statistically significant reduction (P < 0.01).
Showed no significant differences in body weight between treatment groups and controls, indicating low systemic toxicity.
Molecular Weight

351.40

Formula

C20H21N3O3
SMILES

COC1=C(C=C(C=C1)NC(C2=CC(CN3C=NC=C3C)=CC=C2)=O)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CL121 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CL121CL 121CL-121Amyloid-βCD47β-amyloid peptideAβAbetaCluster of Differentiation 47MER6OA3human sQCmouse xenograft tumor modelspyroglutamate (pE)-CD47glutaminyl cyclaseHet1AKYSE30 cellsmacrophage-mediated phagocytosishuman gQCMCF-10AMDA-MB-231 cellsInhibitorinhibitorinhibit

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