2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. CCR4 antagonist 2

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.

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CCR4 antagonist 2 Chemical Structure

CCR4 antagonist 2 Chemical Structure

CAS No. : 2206788-99-8

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CCR4 antagonist 2 Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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Description

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively[1].

IC50 & Target

IC50: 40 nM (Ca2+flux); 70 nM (CTX) (CCR4 antagonist 2)[1]
Cellular Effect
Cell Line Type Value Description References
CCRF-CEM IC50
70 nM
Compound: Example 31
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo as
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo as
[PMID: 31259550]
Molecular Weight

511.45

Formula

C26H28Cl2N6O
CAS No.
SMILES

ClC(C=C(Cl)C=C1)=C1[C@@H](C)N2N=C(C#N)C3=C2N=C(C4=CC[C@H](N5[C@H](CO)CCC5)[C@H](C)C4)C=N3
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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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CCR4 antagonist 2 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:

CCR4 antagonist 22206788-99-8CCRCC chemokine receptorInhibitorinhibitorinhibit

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