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IT1t dihydrochloride

Catalog #: 4596
7 Citations Datasheet
Catalog # Availability Size / Price Qty
4596/10
4596/50
IT1t dihydrochloride | CAS No. 1092776-63-0 | Chemokine Receptor Antagonists
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Description: Potent CXCR4 antagonist

Chemical Name: N,N'-Dicyclohexylcarbamimidothioic acid (5,6-dihydro-6,6-dimethylimidazo[2,1-b]thiazol-3-yl)methyl ester dihydrochloride

Purity: ≥99%

Product Details
Citations (7)
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Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

IT1t dihydrochloride is a potent CXCR4 antagonist (IC50 = 1.1 nM in calcium mobilization assays). Orally available. Blocks interaction with the HIV envelope protein, gp120 (IC50 = 7 nM, inhibition of X4-tropic HIV-1IIIB attachment).

Technical Data

M.Wt:
479.57
Formula:
C21H34N4S2.2HCl
Solubility:
Soluble to 10 mM in DMSO and to 100 mM in water
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
1092776-63-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors
    A Van Hout, T D'huys, M Oeyen, D Schols, T Van Loy
    PLoS ONE, 2017;12(4):e0176057.
  2. Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.
    Thoma et al.
    J.Med.Chem., 2008;51:7915

Product Datasheets

Citations for IT1t dihydrochloride

The citations listed below are publications that use Tocris products. Selected citations for IT1t dihydrochloride include:

7 Citations: Showing 1 - 7

  1. Cell surface thermal proteome profiling tracks perturbations and drug targets on the plasma membrane.
    Authors: Mathias Et al.
    Nat Methods  2021;18:84-91
  2. Kinetic Analysis of the Early Signaling Steps of the Human Chemokine Receptor CXCR4.
    Authors: Martin J Et al.
    Mol Pharmacol  2020;98:72-87
  3. Monitoring Allosteric Interactions with CXCR4 Using NanoBiT Conjugated Nanobodies.
    Authors: Martine J Et al.
    Cell Chem Biol  2020;27:1250-1261.e5
  4. Microtiter plate-based antibody-competition assay to determine binding affinities and plasma/blood stability of CXCR4 ligands.
    Authors: Ludger Et al.
    Sci Rep  2020;10:16036
  5. CRISPR-Mediated Protein Tagging with Nanoluciferase to Investigate Native Chemokine Receptor Function and Conformational Changes.
    Authors: White Et al.
    Cell Chem Bio  2020;
  6. Control of TLR7-mediated type I IFN signaling in pDCs through CXCR4 engagement-A new target for lupus treatment.
    Authors: Smith Et al.
    Sci Adv  2019;5:eaav9019
  7. Characterization, Dynamics, and Mechanism of CXCR4 Antagonists on a Constitutively Active Mutant.
    Authors: Yung-Chi Et al.
    Cell Chem Biol  2019;26:662-673.e7

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