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

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

G4/HDAC-IN-1 Chemical Structure

CAS No. : 3031784-60-5

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G4/HDAC-IN-1 Related Antibodies

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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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)

Cellular Effect
Cell Line Type Value Description References
BT-549 IC50
6.5 μM
Compound: a6
Cytotoxicity against human BT-549 cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability
Cytotoxicity against human BT-549 cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability
[PMID: 36053318]
MDA-MB-231 IC50
4.1 μM
Compound: a6
Cytotoxicity against human MDA-MB-231 cells harboring wild type BRCA1 and wild BRCA2 assessed as reduction in cell viability
Cytotoxicity against human MDA-MB-231 cells harboring wild type BRCA1 and wild BRCA2 assessed as reduction in cell viability
[PMID: 36053318]
MDA-MB-468 IC50
3.3 μM
Compound: a6
Cytotoxicity against human MDA-MB-468 cells harboring wild type BRCA1 and BRCA2 mutant reduction in assessed as cell viability
Cytotoxicity against human MDA-MB-468 cells harboring wild type BRCA1 and BRCA2 mutant reduction in assessed as cell viability
[PMID: 36053318]
SUM-159-PT IC50
7.4 μM
Compound: a6
Cytotoxicity against human SUM159PT cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability
Cytotoxicity against human SUM159PT cells harboring wild type BRCA1 and wild type BRCA2 assessed as reduction in cell viability
[PMID: 36053318]
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].

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

G4/HDAC-IN-1 Related Antibodies

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].

MedChemExpress (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
CAS No.
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
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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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G4/HDAC-IN-1 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:

G4/HDAC-IN-13031784-60-5HDACG-quadruplexHistone deacetylasesdual-targetTNBCanti-tumornuclear extractPu22HRASHTG21MDA-MB-231micexenograftInhibitorinhibitorinhibit

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