MC2590

Cat. No.: HY-152226: FAQs
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MC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) with IC₅₀s of 0.015 μM-0.156 μM. MC2590 also inhibits HDAC isoforms HDAC4, HDAC5, HDAC7, HDAC9, HDAC11 with IC₅₀s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction.

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

MC2590 Chemical Structure

CAS No. : 2284460-01-9

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View All Isoforms

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

HDAC1

0.098 μM (IC₅₀)

HDAC2

0.156 μM (IC₅₀)

HDAC3

0.039 μM (IC₅₀)

HDAC6

0.015 μM (IC₅₀)

HDAC8

0.047 μM (IC₅₀)

HDAC10

0.071 μM (IC₅₀)

HDAC4

2.73 μM (IC₅₀)

HDAC5

1.35 μM (IC₅₀)

HDAC7

2.06 μM (IC₅₀)

HDAC9

2.79 μM (IC₅₀)

HDAC11

3.98 μM (IC₅₀)

In Vitro

MC2625 (compound 5e) has antiproliferative activity with Colorectal carcinoma HCT116 (IC₅₀=0.07 μM), Lung adenocarcinoma A549 (IC₅₀=0.32 μM), Chronic myelogenous leukaemia K562 (IC₅₀=0.05 μM) for 72 h^[1].
MC2625 (1, 5 μM; 24, 48 h) displays mainly G2/M cell cycle arrest^[1].
MC2625 (1, 5 μM; 24, 48 h) reveals H3K9/14 hyperacetylation activity, increases the acetyl-α-tubulin level, markedly upregulates the p21 protein^[1].
MC2625 (1, 5 μM; 48 h) increases mRNA expression of p21, BAX and BAK, downregulates cyclin D1 and BCL-2 and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	Human acute myeloid leukaemia U937 cells
Concentration:	1, 5 μM
Incubation Time:	24, 48 h
Result:	At 24 h, showed very low increase of the pre-G1 peak and led to a G2/M phase arrest at 1 μM; induced a 10% pre-G1 increase and displayed a block at the G2/M phase at 5 μM. At 48 h, induced a 70-85% block of the cell cycle at the G1 phase.

Western Blot Analysis^[1]

Cell Line:	Human acute myeloid leukaemia U937 cells
Concentration:	1, 5 μM
Incubation Time:	24, 48 h
Result:	At 1 μM revealed H3K9/14 hyperacetylation activity, increased the acetyl-α-tubulin level, markedly upregulated the p21 protein.

RT-PCR^[1]

Cell Line:	Human acute myeloid leukaemia U937 cells
Concentration:	1, 5 μM
Incubation Time:	48 h
Result:	At 1 μM significantly induced the expression of BAX and BAK, dose-dependently downregulated the antiapoptotic factor BCL-2. Downregulated miRNAs with antiapoptotic activity (miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p, miR-21-5p); induced the proapoptotic miRNAs (miR-let7a-5p, miR-125b-5p, miR-181a-5p, miR-181b-5p, miR-769-5p, miR-122-5p).

Molecular Weight

347.37

Formula

C₂₀H₁₇N₃O₃

CAS No.

2284460-01-9

SMILES

O=C(NO)/C=C/C1=NC=C(C=C1)NC(CC2=C3C=CC=CC3=CC=C2)=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

Handling Instructions (2659 KB)

References

[1]. Elisabetta Di Bello, et al. Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells. Eur J Med Chem. 2022 Dec 15;247:115022. [Content Brief]

MC2590 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.

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