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HDAC-IN-48

HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI₅₀~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins. HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

CAS No.: 3031411-05-6
Formula: C₁₃H₁₇N₃O₃S
Molecular Weight:295.36

Storage:

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

Data Sheet (268 KB)

HDAC-IN-48 Chemical Structure

CAS No.: 3031411-05-6

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

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

Biological Activity

Description

HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI₅₀~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins^[1]. HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

All HDAC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.61 μM Compound: HY-1	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 30 mins by methylene blue staining based analysis Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 30 mins by methylene blue staining based analysis	[PMID: 36306372]
NCI-H23	GI₅₀	0.78 μM Compound: HY-1	Cytotoxicity against human NCI-H23 cells assessed as cell growth inhibition at 10 uM incubated for 24 hrs by MTT assay Cytotoxicity against human NCI-H23 cells assessed as cell growth inhibition at 10 uM incubated for 24 hrs by MTT assay	[PMID: 36306372]
NCI-H522	IC₅₀	0.5 μM Compound: HY-1	Cytotoxicity against human NCI-H522 cells assessed as reduction in cell viability incubated for 30 mins by methylene blue staining based analysis Cytotoxicity against human NCI-H522 cells assessed as reduction in cell viability incubated for 30 mins by methylene blue staining based analysis	[PMID: 36306372]
RPMI-8226	GI₅₀	0.35 μM Compound: HY-1	Cytotoxicity against human RPMI-8226 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human RPMI-8226 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 36306372]
SF-539	GI₅₀	1 μM Compound: HY-1	Cytotoxicity against human SF-539 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human SF-539 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 36306372]
WI-38	IC₅₀	8.37 μM Compound: HY-1	Cytotoxicity against human WI-38 cells assessed as reduction in cell survival incubated for 30 mins by methylene blue staining based analysis Cytotoxicity against human WI-38 cells assessed as reduction in cell survival incubated for 30 mins by methylene blue staining based analysis	[PMID: 36306372]

In Vitro

HDAC-IN-48 (0-40 μM; 3 d) has superior antiproliferative activity on cancer cells (NCI-H522 and HCT-116) vs the normal cells (WI38 and RPE) with IC₅₀s of 0.5 μM (NCI-H522), 0.61 μM (HCT-116), 8.37 μM (WI38, normal human lung fibroblasts), and 6.13 μM (RPE, retinal pigment epithelial cells), respectively^[1].
HDAC-IN-48 (2.5 μM; 24 h) suppresses cell viability by inducing ferroptosis and HDAC inhibition^[1].
HDAC-IN-48 (10 μM; 6 h) decreases the lipid peroxide level compared with SAHA^[1].
HDAC-IN (0.58 μM, 1.16 μM, and 2.32 μM; 3 d) has no neurotoxic effects and (2.5, 5, and 10 μM; 3 d) leads to hyper acetylation of histones and tubulin^[1].
Nondifferentiated PC-12 cells have stem-like properties, but when differentiated by a nerve growth factor, they demonstrate neuronal behavior. HDAC-IN-48 (0.58 μM, 1.16 μM, and 2.32 μM; 24 h) behaves as the HDAC control effect, shows few ferroptosis induction on both differentiated and undifferentiated PC-12 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

NCI-H522 cells
Concentration:

2.5, 5, and 10 μM
Incubation Time:

72 hours; at the corresponding concentrations in the presence of Liproxstatin-1 (0.25 μM)
Result:

Led to hyperacetylation of histones and tubulin in a similar way to SAHA (pan-inhibitor).

Cell Viability Assay^[1]

Cell Line:

NCI-H522, WI38, HCT-116, and RPE
Concentration:

0-40 μM
Incubation Time:

72 hours
Result:

Showed selectivity among normal cells over cancer cells.
Inhibited cell survival with IC50s of 0.5 μM, 8.37 μM, 0.61 μM, and 6.13 μM.

Apoptosis Analysis^[1]

Cell Line:

NCI-H522 cells
Concentration:

5 μM
Incubation Time:

24 hours, 48 hours, and 72 hours
Result:

Induced cell ferroptosis.

Chemical Information

CAS No. 3031411-05-6
Molecular Weight 295.36
Formula C₁₃H₁₇N₃O₃S
SMILES

O=C(C1=CSC(C#C)=N1)NCCCCCCC(NO)=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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 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]. Karaj E, et al. First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids. J Med Chem. 2022 Nov 10;65(21):14764-14791. [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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