1. Cell Cycle/DNA Damage
    Epigenetics
    Autophagy
    Apoptosis
  2. HDAC
    Autophagy
    Apoptosis
  3. HDAC-IN-36

HDAC-IN-36 

Cat. No.: HY-146684
Handling Instructions

HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research.

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

HDAC-IN-36 Chemical Structure

HDAC-IN-36 Chemical Structure

CAS No. : 2482992-54-9

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Description

HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research[1].

IC50 & Target

HDAC6

11.68 nM (IC50)

HDAC10

13.24 nM (IC50)

HDAC3

79.17 nM (IC50)

HDAC1

86.93 nM (IC50)

HDAC2

97.32 nM (IC50)

HDAC8

378.2 nM (IC50)

HDAC4

>1000 nM (IC50)

HDAC5

>1000 nM (IC50)

HDAC7

>1000 nM (IC50)

HDAC9

>1000 nM (IC50)

HDAC11

>1000 nM (IC50)

In Vitro

HDAC-IN-36 (compound 23 g) (0-10, 24 h) exhibits good antiproliferative activity in MDA-MB-231 cells, promotes the acetylation of α-Tubulin and HSP90[1].
HDAC-IN-36 (0-10, 24 h) induces apoptosis in MDA-MB-231 cells in a dose-dependent manner, and mainly induces mitochondrial-dependent apoptosis[1].
HDAC-IN-36 (0-10, 24 h) inhibits MDA-MB-231 cells migration in a dose-dependent manner, increases the expression of E-cadherin and decreases the expression of MMP-2 obviously[1].
HDAC-IN-36 (0-10, 24 h) induces noteworthy autophagy, increases the expression of Beclin1, LC3II and decreases the expression of SQSTM1/p62[1].

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

Cell Viability Assay

Cell Line: MDA-MB-231 cells[1]
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Exhibited good anti-proliferative activity in MDA-MB-231 cells, with IC50 of 1.32 ± 0.13 μM, increased the acetylation level of intracellular proteins, and promoted the acetylation of α-Tubulin and HSP90.

Apoptosis Analysis

Cell Line: MDA-MB-231 cells[1]
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced apoptosis in MDA-MB-231 cells in a dose-dependent manner.

Cell Autophagy Assay

Cell Line: MDA-MB-231 cells[1]
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced noteworthy autophagy with increased aggregation of LC3 puncta.

Western Blot Analysis

Cell Line: MDA-MB-231 cells[1]
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Mainly induced mitochondrial-dependent apoptosis, up-regulated the expression of Bax and downregulated the expression of Bcl-2, and increased the cleavage of caspase3, caspase8 and caspase9; increased the expression of E-cadherin and decreased the expression of MMP-2 obviously; increased the expression of Beclin1, LC3II and decreased the expression of SQSTM1/p62.
In Vivo

HDAC-IN-36 (compound 23 g) (Zebrafish tumor xenograft model; 0-5 μg/mL, 3 days) shows potent anti-tumor and anti-metastatic activity, and improves in vivo anti-tumor efficacy[1].
HDAC-IN-36 (Beagles, 20 mg/kg, Orally, once) shows a significant improvement in pharmacokinetic parameters[1].
Pharmacokinetic Parameters of HDAC-IN-36 in male Beagles[1].

Parameters 23g (20 mg/kg)
T1/2 (h) 1.24 ± 0.21
Tmax (h) 0.79 ± 0.33
Cmax (μg/L) 120.36 ± 15.53
AUC0-t (μg/L∗h) 1275.35 ± 70.17
AUC0-∞ (μg/L∗h) 1289.40 ± 88.91

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

Animal Model: Zebrafish (MDA-MB-231-derived xenograft model, Wild-type AB strain)[1]
Dosage: 0, 2.5, 5 μg/mL
Administration: 3 days
Result: Inhibited tumor formation and migration in a dose-dependent manner, and improved in vivo anti-tumor efficacy.
Animal Model: Beagles (female, 8-10 kg, n = 4)[1]
Dosage: 20 mg/kg (dissolved 0.5% sodium carboxyl methyl cellulose (CMC-Na) aqueous solution)
Administration: Orally, once (Pharmacokinetic Analysis)
Result: Showed a significant improvement in pharmacokinetic parameters with T1/2 value of 1.24 h.
Molecular Weight

537.65

Formula

C29H39N5O5

CAS No.
SMILES

COC1=CC(OC)=C2C(N=C(N=C2N3CCN(CC3)C)C4=CC(C)=C(C(C)=C4)OCCCCCC(NO)=O)=C1

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-36
Cat. No.:
HY-146684
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