2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC-IN-89

HDAC-IN-89 is an inhibitor of HDAC1 (IC50: 0.95 nM), HDAC2 (IC50: 0.86 nM), HDAC3 (IC50: 1.06 nM) and HDAC8 (IC50: 4.24 nM). HDAC-IN-89 blocks the cell cycle and induces apoptosis. HDAC-IN-89 has anti-tumor activity.

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

HDAC-IN-89 Chemical Structure

HDAC-IN-89 Chemical Structure

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HDAC-IN-89 Related Antibodies

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Description

HDAC-IN-89 is an inhibitor of HDAC1 (IC50: 0.95 nM), HDAC2 (IC50: 0.86 nM), HDAC3 (IC50: 1.06 nM) and HDAC8 (IC50: 4.24 nM). HDAC-IN-89 blocks the cell cycle and induces apoptosis. HDAC-IN-89 has anti-tumor activity[1].

IC50 & Target[1]

HDAC1

0.95 nM (IC50)

HDAC2

0.86 nM (IC50)

HDAC3

1.06 nM (IC50)

HDAC8

4.24 nM (IC50)

HDAC6

>1000 nM (IC50)

In Vitro

HDAC-IN-89 (Compound 12) (0-10000 nM, 72 h) shows cytotoxicity against both NCI-H1975 (IC50: 0.57 μM) and HT-29 (IC50: 0.17 μM) cancer cells, but shows significantly reduced cytotoxicity against both WRL-68 (IC50: 2.6 μM) and HEK293 (IC50: 1.0 μM) normal cells[1].
HDAC-IN-89 (250 nM-1 μM, 48 h) induces cell cycle arrest in the G0/G1 phase of HT-29 cells and significantly promotes apoptosis of early and late cells at the corresponding concentrations[1].
HDAC-IN-89 (0-40 μM) has a small inhibitory effect on the hERG potassium channel (21%), indicating a low risk of cardiotoxicity[1].
HDAC-IN-89 (0.1 μM, 7-60 min) shows moderate metabolic stability (MF%: 30%-70%) and rapid clearance (Clint: 21.7-43.7 mL/min/g) in mouse, rat and human liver microsomes[1].

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

HDAC-IN-89 Related Antibodies

Cell Viability Assay[1]

Cell Line: Tumor cells (NCI-H1975 cells, HT-29 cells) and normal cells (WRL-68 cells, HEK293 cells)
Concentration: 0-10000 nM
Incubation Time: 72 h
Result: Inhibited the activity of two cancer cells, NCI-H1975 (IC50: 0.57 μM) and HT-29 (IC50: 0.17 μM).
Reduced the toxicity to two normal cells, WRL-68 (IC50: 2.6 μM) and HEK293 (IC50: 1.0 μM).

Cell Cycle Analysis[1]

Cell Line: HT-29 cells
Concentration: 250 nM, 500 nM and 1μM
Incubation Time: 48 h
Result: Induced cell cycle arrest in HT-29 cells at the G0/G1 phase (%G0/G1: 55.0%/57.2%/74.0%).

Apoptosis Analysis[1]

Cell Line: HT-29 cells
Concentration: 250 nM and 500 nM
Incubation Time: 48 h
Result: Promoted apoptosis of early cells (14.3%/19.7%) and late cells (7.57%/11.1%) at the corresponding concentrations (250 nM/500 nM).
In Vivo

HDAC-IN-89 (Compound 12) (2.2 mg/kg and 11 mg/kg, IP, once every 3 days for 21 days) inhibits tumor growth (63.5% and 87.9%) in the mouse NCI-H1975 xenograft model and shows low toxicity[1].

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

Animal Model: NCI-H1975 xenograft model[1]
Dosage: 2.2 mg/kg and 11 mg/kg
Administration: Intraperitoneal injection (i.p.), once every 3 days for 21 days
Result: Inhibited tumor growth (63.5% and 87.9%).
Had no significant changes in body weight compared to the same dose of Romidepsin (2.2 mg/kg).
Molecular Weight

575.69

Formula

C24H35F2N5O5S2
SMILES

CC(C)[C@@H](C(N[C@H](/C=C/CCSSC[C@@H](C1=O)NC2=O)C(F)(F)C(N[C@@H]2C(C)C)=O)=O)NC(/C(N1)=C/C)=O
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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HDAC-IN-89 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:

HDAC-IN-89HDACHistone deacetylasesAnti-tumorNCI-H1975HT-29hERG potassium channelNCI-H1975 xenograft modelInhibitorinhibitorinhibit

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