1. Metabolic Enzyme/Protease Stem Cell/Wnt MAPK/ERK Pathway Immunology/Inflammation
  2. IFNAR Interleukin Related Tyrosinase ERK
  3. RDN2150

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.

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RDN2150

RDN2150 Estructura química

No. CAS : 2839429-51-3

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Top Publications Citing Use of Products

1 Publications Citing Use of MCE RDN2150

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Descripciòn

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[1][2].

IC50 & Target

14.6 nM (ZAP-70)[1]

Cellular Effect
Cell Line Type Value Description References
Splenocyte IC50
64 nM
Compound: 25; RDN2150
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
[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.

Western Blot Analysis[2]

Cell Line: Jurkat T cells (JOT1 and CD19-CAR Jurkat sublines)
Concentration: 0.1 μM; 1 μM; 10 μM; 100 nM
Incubation Time: 3 h
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

RDN2150 (2%; topical; once daily; 7 days) significantly reduces psoriasis-like skin lesions and splenomegaly in an Imiquimod (HY-B0180)-induced mouse model of psoriasis[1].

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

Animal Model: BALB/c (female, 6-8 weeks old, 18-20 g, Imiquimod-induced psoriasis-like dermatitis)[1]
Dosage: 2% (62.5 mg per application)
Administration: topical; once daily; 7 days
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.
Peso molecular

577.03

Fòrmula

C28H29ClN8O4

No. CAS
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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación
Referencias
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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.

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Inquiry Information

Nombre del producto:
RDN2150
Cat. No.:
HY-155978
Cantidad:
MCE Japan Authorized Agent: