2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. MC2590

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.

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MC2590 Chemical Structure

MC2590 Chemical Structure

CAS No. : 2284460-01-9

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MC2590 Related Antibodies

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

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Description

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[1].

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.

MC2590 Related Antibodies

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.
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
References
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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.

Keywords:

MC25902284460-01-9MC 2590MC-2590HDACApoptosisHistone deacetylasesPyridinehistone deacetylaseHDAC1HDAC2HDAC3HDAC6HDAC8HDAC10class I/IIbHDAC4HDAC5HDAC7HDAC9HDAC11G2/MmicroRNAsp21BAXBAKInhibitorinhibitorinhibit

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