1. Cell Cycle/DNA Damage
    Epigenetics
    Cytoskeleton
    Apoptosis
  2. HDAC
    Microtubule/Tubulin
    Apoptosis
  3. HDAC-IN-9

HDAC-IN-9 

Cat. No.: HY-115941
Handling Instructions

HDAC-IN-9 is a potent and selective tubulin and HDAC dual inhibitor. HDAC-IN-9 inhibits the invasion and migration of A549 cells. HDAC-IN-9 shows potent antitumor and antiangiogenic effect in vitro and in vivo.

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

HDAC-IN-9 Chemical Structure

HDAC-IN-9 Chemical Structure

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Description

HDAC-IN-9 is a potent and selective tubulin and HDAC dual inhibitor. HDAC-IN-9 inhibits the invasion and migration of A549 cells. HDAC-IN-9 shows potent antitumor and antiangiogenic effect in vitro and in vivo[1].

IC50 & Target[1]

HDAC1

6.8 μM (IC50)

HDAC2

0.06 μM (IC50)

HDAC6

0.12 μM (IC50)

HDAC8

8.5 μM (IC50)

In Vitro

HDAC-IN-9 (compound 4s) shows anti-proliferative activity (IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, 0.371 µM for MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells, respectively)[1].
HDAC-IN-9 displays 6.1, 3.2 and 4.6-fold selectivity ratios for 293 T, macrophages, and L02 cells respectively (IC50s of 10.89, 5.63, 8.14 µM for 293 T, macrophages, and L02 cells, respectively)[1].
HDAC-IN-9 shows inhibition activities against HDAC isoforms (IC50s of 6.8, 0.06, 0.12, 8.5 µM for HDAC 1, HDAC 2, HDAC 6, HDAC 10, respectively)[1].
HDAC-IN-9 (1, 2, 4 µM; 72 h; A459 cells) induces cell cycle arrest at the G2/M phase in a concentration-dependent manner[1].
HDAC-IN-9 (1, 2, 4 µM; 72 h) induces apoptosis via a Caspase-dependent intrinsic mitochondrial-mediated pathway in A549 cells[1].
HDAC-IN-9 (0, 0.5, 1, 2 µM; 48 h) shows anti-proliferative activity by the inhibition of angiogenesis and the reduction of endothelial cell metastasis in A549 cells[1].
HDAC-IN-9 (0, 1, 2, 4 µM, 48 h) inhibits the invasion and migration of A549 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferative activity (IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, 0.371 µM for MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells, respectively).

Cell Cycle Analysis[1]

Cell Line: A459 cells
Concentration: 0, 1, 2, 4 µM
Incubation Time: 72 h
Result: Cells were arrested at the G2/M phase with a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: A459 cells
Concentration: 0, 1, 2, 4 µM
Incubation Time: 72 h
Result: Induced apoptosis via a Caspase-dependent intrinsic mitochondrial-mediated pathway in A549 cells.

Western Blot Analysis[1]

Cell Line: A459 cells
Concentration: 0, 1, 2, 4 µM
Incubation Time: 72 h
Result: Showed down regulation of Cyclin B1 and Pcdc2 levels.
In Vivo

HDAC-IN-9 (0, 10, 20, 40 µM) suppresses the formation of intersegmental blood vessels (ISVs) in zebrafish embryos[1].
HDAC-IN-9 (0, 2.5, 5, 10 µM; 3 days) inhibits the proliferation and metastasis of A549 cells in zebrafish xenograft models[1].

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

Animal Model: embryos of Tg(flk:EGFP) transgenic zebrafish (transgenic zebrafish model Tg(flk1:EGFP))[1]
Dosage: 0, 10, 20, 40 µM
Administration:
Result: Suppressed the formation of ISVs in zebrafish embryos.
Animal Model: zebrafish xenograft models[1]
Dosage: 0, 2.5, 5, 10 µM
Administration: 3 days
Result: Inhibited the proliferation and metastasis of A549 cells in zebrafish xenograft models.
Molecular Weight

526.67

Formula

C33H38N2O4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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HDAC-IN-9
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HY-115941
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