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HDAC-IN-73

HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC₅₀s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC₅₀=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer .

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

CAS No.: 2323571-16-8
Formula: C₂₂H₂₄Br₂N₄O₆Se₂
Molecular Weight:758.18

Storage:

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

Data Sheet (272 KB)

HDAC-IN-73 Chemical Structure

CAS No.: 2323571-16-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

HDAC1

0.17 μM (IC₅₀)

HDAC6

0.49 μM (IC₅₀)

All HDAC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.03 μM Compound: 9	Cytotoxicity against human A549 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human A549 cells assessed as reduction in cell viability by SRB assay	[PMID: 33636429]
HCT-116	IC₅₀	0.01 μM Compound: 9	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay	[PMID: 33636429]
HCT-116	IC₅₀	0.24 μM Compound: P-503	Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by MTT assay	[PMID: 38851056]
MCF-10A	IC₅₀	16.14 μM Compound: 9	Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability by SRB assay	[PMID: 33636429]
MDA-MB-231	IC₅₀	0.16 μM Compound: 9	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by SRB assay	[PMID: 33636429]
SK-HEP1	IC₅₀	0.21 μM Compound: 9	Cytotoxicity against human SK-HEP1 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human SK-HEP1 cells assessed as reduction in cell viability by SRB assay	[PMID: 33636429]
SNU-638	IC₅₀	0.02 μM Compound: 9	Cytotoxicity against human SNU-638 cells assessed as reduction in cell viability by SRB assay Cytotoxicity against human SNU-638 cells assessed as reduction in cell viability by SRB assay	[PMID: 33636429]

In Vitro

HDAC-IN-73 (compound P-503) (0-10 µM; 48 h) can inhibit proliferation of HCT116 cells with IC₅₀ value of 0.24 µM while PsA’s IC₅₀ value is 3.05 µM^[1].
HDAC-IN-73 (0.25-2 µM; 24 h) can increase the acetylation levels of histone H3 or α-tubulin in HCT116 cells comparing with PsA^[1].
HDAC-IN-73 (0.1-0.2 µM; 24 h) can induce apoptosis of HCT116 cells and has a superior proapoptotic effect to PsA^[1].
HDAC-IN-73(0.2-0.4 µM; 48 h) can induce HCT116 cell cycle arrest at G2 / M phase while PsA increases proportion of G1 phase^[1].

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

Apoptosis Analysis^[1]

Cell Line:

HCT116 cells
Concentration:

0.2, 0.4 µM
Incubation Time:

48 hours
Result:

Induced apoptosis with 71.94 % of apoptotic cells (both early and late apoptotic cells) at define concentration of 0.4 μM, compared with PsA (56.5 %, 4 μM) .

Cell Cycle Analysis^[1]

Cell Line:

HCT116 cells
Concentration:

0.1, 0.2 µM
Incubation Time:

24 hours
Result:

Induced cell cycle arrest at G2 / M phase while PsA increased proportion of G1 phase. HDAC-IN-73 with 0.1 μM and 0.2 μM can lead to 47.92 % and 74.56 % of the cells in G2 / M phase, respectively.

Western Blot Analysis^[1]

Cell Line:

HCT116 cells
Concentration:

0.25, 0.5, 1, 2 µM
Incubation Time:

24 hours
Result:

Increased the acetylation levels of histone H3 or α-tubulin in a dose dependent manner comparing with PsA.

In Vivo

HDAC-IN-73 (compound P-503)(5 mg/kg; i.p.; every 2 days for 26 days) demonstrates a notable antitumor activity but also exists higher toxicity in HCT116 xenograft model in a 5 mg/kg dosage. The safety and toxic doses of HDAC-IN-73 needs further investigation^[1].

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

Animal Model:

6 weeks, Female nude mice (BALB/c-nu) (HCT116 xenograft model)^[1]
Dosage:

5 mg/kg
Administration:

I.p.; every 2 days for 26 days
Result:

Reduced the tumor volume (p < 0.0001) and the tumor weight (p < 0.01). Exhibited the significant loss of body weight which has the same trend with the group of negative control. Inhibited the tumor growth (TGI = 74.6 %) , while the TGI of SAHA (10 mg/kg, positive control) and PsA (10 mg/kg) were 13.1 % and 36.1 %, respectively.
Existed high toxicity, 2 mice died during the medication. Western blot tests showed that the acetylation levels of histone H3 or α-tubulin in tumor tissues were up-regulated.

Chemical Information

CAS No. 2323571-16-8
Molecular Weight 758.18
Formula C₂₂H₂₄Br₂N₄O₆Se₂
SMILES

OC1=CC=C(C/C(C(NCC[Se][Se]CCNC(/C(CC2=CC=C(O)C(Br)=C2)=N/O)=O)=O)=N\O)C=C1Br
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jiang Y, et al. Psammaplin A analogues with modified disulfide bond targeting histone deacetylases: Synthesis and biological evaluation. Eur J Med Chem. 2024 May 31;275:116541. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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