1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
    G-quadruplex
  3. G4/HDAC-IN-1

G4/HDAC-IN-1 

Cat. No.: HY-151263
Handling Instructions

G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer.

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

G4/HDAC-IN-1 Chemical Structure

G4/HDAC-IN-1 Chemical Structure

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Description

G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer[1].

IC50 & Target

HDAC8

0.03 μM (IC50)

HDAC6

0.65 μM (IC50)

HDAC1

1.26 μM (IC50)

HDAC11

1.38 μM (IC50)

HDAC4

2.64 μM (IC50)

In Vitro

G4/HDAC-IN-1 (0-10 μM; 1.5 h) shows HDAC inhibitory activity with an IC50 of 1.9 μM by determining nuclear extract and exhibits inhibitory activity on intracellular HDAC activity in MDA-MB-231 cells with an IC50 value of 1.1 μM[1].
G4/HDAC-IN-1 (0-50 μM) shows G4 binding activity with an IC50 of 0.4 μM[1].
G4/HDAC-IN-1 (0-10 μM; 1.5 h) inhibits HDAC1, HDAC8, HDAC4, HDAC6 and HDAC11 activities with IC50s of 1.26, 0.03, 2.64, 0.65 and 1.38 μM, respectively[1].
G4/HDAC-IN-1 (0-50 μM) binds with Pu22, HRAS and HTG21 sequences with KD values of 1.8, 3.6 and >10 μM, respectively[1].
G4/HDAC-IN-1 (1.25-5.0 μM; 48 h) dose-dependently increases DNA G4 level[1].
G4/HDAC-IN-1 (0-50 μM; overnight) inhibits cytotoxic activities of TNBC cell lines[1].

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

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cell line
Concentration: 1.25, 2.5 and 5.0 μM
Incubation Time: 48 hours
Result: Increased the acetylation levels of HDAC1/2/3/8 substrate acetyl histone H3 (ac-H3), acetyl-histone H4 (ac-H4), and the HDAC6 substrate acetyl-α-tubulin (ac-Tub).

Cell Cytotoxicity Assay[1]

Cell Line: TNBC cell lines
Concentration: 0-50 μM
Incubation Time: Overnight
Result: Showed cytotoxic activities to MDA-MB-231, MDA-MB-468, SUM159PT and BT549 with IC50s of 4.1, 3.3, 7.4 and 6.5 μM, respectively.
In Vivo

G4/HDAC-IN-1 (2.5 mg/kg; i.p. once daily for 31 days) shows antitumor activity[1].

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

Animal Model: Five week-old female BALB/C mice with TNBC xenografts[1]
Dosage: 2.5 mg/kg
Administration: Intraperitoneal injection; 2.5 mg/kg once daily; for 31 days
Result: Showed well tolerance in vivo and exhibited potent antitumor activity.
Molecular Weight

698.27

Formula

C36H49ClFN7O4

SMILES

O=C(NCCCN(C)C)C1=CC=C(/C=C2CCN3C\2=NC4=C(C=C(F)C(N5CCN(CCCCCCCC(NO)=O)CC5)=C4)C3=O)C=C1.Cl

Shipping

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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Product Name:
G4/HDAC-IN-1
Cat. No.:
HY-151263
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