1. GPCR/G Protein Immunology/Inflammation
  2. CXCR
  3. UCUF-965

UCUF-965 is a CXCR4 positive allosteric modulator. UCUF-965 potentiates CXCL12-induced β-arrestin recruitment and cAMP signaling, activates lymphoblast migration, induces calcium flux, and does not bind CXCR4’s orthosteric CXCL12 site. UCUF-965 reduces miR-15b and miR-29a levels, increases miR-146a levels in fibroblasts. UCUF-965 enhances angiogenesis and reduces wound healing time in diabetic mice. UCUF-965 can be used for the research of diabetic wound healing impairment.

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UCUF-965

UCUF-965 Chemical Structure

CAS No. : 2965316-77-0

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Description

UCUF-965 is a CXCR4 positive allosteric modulator. UCUF-965 potentiates CXCL12-induced β-arrestin recruitment and cAMP signaling, activates lymphoblast migration, induces calcium flux, and does not bind CXCR4’s orthosteric CXCL12 site. UCUF-965 reduces miR-15b and miR-29a levels, increases miR-146a levels in fibroblasts. UCUF-965 enhances angiogenesis and reduces wound healing time in diabetic mice. UCUF-965 can be used for the research of diabetic wound healing impairment[1].

IC50 & Target[1]

CXCR4

 

In Vitro

UCUF-965 (0.1-10 μM) promotes β-arrestin recruitment with an EC50 of 0.02 μM[1].
UCUF-965 acts as a partial agonist of CXCR4-mediated cAMP inhibition in CXCR4-overexpressing CHO cells, with an EC50 of 0.05 μM[1].
UCUF-965 (0.4 μM; 3 h) induces migration of CEM-CCRF human lymphoblast cells via CXCR4 activation, with an EC50 of 0.4 μM[1].
UCUF-965 (10 μM) induces CXCR4-mediated calcium flux in CEM-CCRF human lymphoblast cells[1].
UCUF-965 (0.1-10 μM; 24 h) modulates the expression of wound healing-related microRNAs in murine diabetic and non-diabetic fibroblasts, reducing miR-15b and miR-29a levels and increasing miR-146a levels[1].

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

Cell Migration Assay [1]

Cell Line: CEM-CCRF human lymphoblast cells
Concentration: 0.4 μM
Incubation Time: 3 h
Result: Induced CEM-CCRF cell migration with an EC50 of 0.4 μM and an average Eₘₐₓ of 31%.

Real Time qPCR[1]

Cell Line: murine diabetic (Db/Db) fibroblasts; murine non-diabetic (HZ) fibroblasts
Concentration: 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Decreased the expression of miR-15b in both diabetic and non-diabetic fibroblasts in a dose-dependent manner.
Decreased miR-29a levels and increased miR-146a levels in both cell types, with responses observed at concentrations as low as 0.1 μM.
In Vivo

UCUF-965 (10 μM; intradermal injection; single dose) reduces diabetic wound healing time by 36% and enhances angiogenesis in diabetic mice[1].

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

Animal Model: Db/Db mice (10-week-old female, diabetic model)[1]
Dosage: 10 μM
Administration: intradermal injection; single dose (immediately after wounding)
Result: Reduced wound surface area compared to controls starting at post-injury day 6.
Achieved full wound closure at day 14, representing a 36% reduction in wound healing time compared to day 22 in PBS-treated controls.
Showed a significant increase in CD31-positive endothelial cells at day 7 post-wounding, reaching levels similar to non-diabetic control wounds.
Molecular Weight

405.52

Formula

C22H23N5OS

CAS No.
SMILES

N=1N=C(C=2C=CC=CC2OCC)N3N=C(C=4C=CC(=CC4)N5CCCC5)CSC13

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Room temperature in continental US; may vary elsewhere.

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

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    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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UCUF-965
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HY-182850
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