RDN2150
Based on 1 publication(s) in Google Scholar
RDN2150 is a ZAP-70 inhibitor with an IC50 of 14.6 nM, and it exhibits selectivity for Syk over other kinases. RDN2150 inhibits signal transduction and activation of T cells/CAR-T cells, reduces the phosphorylation level of Erk1/2, suppresses the induction of CD69 and IL-2, and downregulates phosphotyrosine signaling pathways including hnRNP sites in T cells. RDN2150 can be used for psoriasis-related research.
The free form of the compound is prone to instability, it is advisable to consider the stable salt form (RDN2150 TFA) that retains the same biological activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2839429-51-3
- Formel: C28H29ClN8O4
- Molecular Weight:577.03
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Other In-stock Forms of RDN2150
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Biologische Aktivität
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Chemical Information
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- Reinheit & Dokumentation
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) RDN2150
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Biologische Aktivität
Beschreibung
IC50 & Target
14.6 nM (ZAP-70)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Splenocyte | IC50 |
64 nM
Compound: 25; RDN2150
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Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation incubated for 48 hrs by [3H]-thymidine incorporation based beta scintillation counter analysis
Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation incubated for 48 hrs by [3H]-thymidine incorporation based beta scintillation counter analysis
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[PMID: 37594408] |
In Vitro
RDN2150 (0.1-10 μM; 3 h) blocks LAT Y220 phosphorylation, disrupts the LAT/SLP76 signalosome, and inhibits downstream Erk1/2 and PLCγ1 activation in Jurkat T cells[2].
RDN2150 (0.1-10 μM; 25 h) inhibits T cell activation markers in Jurkat T cells. In soluble antibody, APC-pMHC/TCR and CD19-CAR/Raji stimulation models, concentrations of 0.1-10 μM reduce CD69 expression and IL-2 secretion, while a concentration of 10 μM completely abrogates soluble antibody-induced CD69 expression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat T cells (JOT1 and CD19-CAR Jurkat sublines)
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Concentration:0.1 μM; 1 μM; 10 μM; 100 nM
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Incubation Time:3 h
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Result:Reduced basal Erk1/2 phosphorylation at 100 nM.
Impaired phosphorylation of LATY220 across all three stimulation methods at 10 μM.
Left phosphorylation of LckY394 unaffected at any concentration.
Significantly reduced phosphorylation of Erk1T202Y204/Erk2T185Y187 at 1 μM and 10 μM after 2.5 min of stimulation across all activation models.
Significantly enhanced PLCγ1Y783 induction after soluble antibody stimulation at low concentrations (0.1 μM, 1 μM).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old, 18-20 g, Imiquimod-induced psoriasis-like dermatitis)[1]
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Dosage:2% (62.5 mg per application)
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Administration:topical; once daily; 7 days
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Result:Significantly reduced cumulative psoriasis severity total score (0-12 scale) compared to vehicle/ointment base controls, with statistically significant differences observed from day 2 onward.
Significantly decreased individual scores for scales, skin thickness, and erythema (0-4 scales each) with statistically significant differences from day 2 onward.
Significantly reduced splenomegaly, resulting in a lower spleen index (spleen weight/body weight) compared to the vehicle group.
Chemical Information
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CAS. Nr. 2839429-51-3
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Molecular Weight 577.03
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Formel C28H29ClN8O4
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SMILES
O=C(C1=C(N=C(N2C1=NC=C2)NCC3=CC(NC(C=C)=O)=C(C=C3)Cl)NC4=CC(OC)=C(C=C4)N5CCOCC5)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Reinheit & Dokumentation
Verweise
[1]. Rao D, et al. Discovery and Structural Optimization of Covalent ZAP-70 Kinase Inhibitors against Psoriasis. J Med Chem. 2023;66(17):12018-12032. [Content Brief]
[2]. Callahan A, et al. Phosphotyrosine proteomics reveals novel Zap70 and Itk pathway targets downstream of TCR and CAR in Jurkat T cells. Sci Rep. 2026;16(1):16482. Published 2026 Apr 6. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
RDN2150 Related Classifications
HY-155978 Related Classifications
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