1. GPCR/G Protein
    Immunology/Inflammation
    Anti-infection
  2. CXCR
    HIV
  3. TC14012

TC14012 

Cat. No.: HY-P1102
Handling Instructions

TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic inverse CXCR4 agonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity.

For research use only. We do not sell to patients.

TC14012 Chemical Structure

TC14012 Chemical Structure

CAS No. : 368874-34-4

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Description

TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic inverse CXCR4 agonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity[1][2].

IC50 & Target[1][2]

CXCR4

19.3 nM (IC50)

CXCR7

350 nM (EC50)

HIV

 

In Vitro

TC14012 (1 mM) inhibits by more than 95% the infection of the CXCR4-expressing cells by the HXB2 (X4) or 89.6 (dual-tropic) strain whereas TC14012 (1 mM) does not inhibit at all the infection of the CCR5-expressing cells by the SF162 (R5) or 89.6 (dualtropic) strain[1].
TC14012 leads to erk 1/2 phosphorylation in U373 cells, which express endogenous CXCR7 but not CXCR4 in U373 cells. Upon stimulation with TC14012, CXCR7 and the CXCR7-Cter4 chimera are able to recruit arrestin, whereas CXCR4 and CXCR4-Cter7 remain silent[2].

Molecular Weight

2066.42

Formula

C₉₀H₁₄₀N₃₄O₁₉S₂

CAS No.

368874-34-4

Sequence

Arg-Arg-{2Nal}-Cys-Tyr-{Cit}-Lys-{Cit}-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2 (Disulfide bridge:Cys4-Cys13)

Sequence Shortening

RR-{2Nal}-CY-{Cit}-K-{Cit}-PYR-{Cit}-CR-NH2 (Disulfide bridge:Cys4-Cys13)

SMILES

[RR-{2Nal}-CY-{Cit}-K-{Cit}-PYR-{Cit}-CR-NH2 (Disulfide bridge:Cys4-Cys13)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

TC14012TC 14012TC-14012CXCRHIVCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency viruserk1/2phosphorylationβ-arrestin2Inhibitorinhibitorinhibit

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TC14012
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HY-P1102
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