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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Based on 1 publication(s) in Google Scholar

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.
Appearance

Solid

Color

Off-white to light yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (287.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8788 mL 14.3939 mL 28.7877 mL
5 mM 0.5758 mL 2.8788 mL 5.7575 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8788 mL 14.3939 mL 28.7877 mL 71.9694 mL
5 mM 0.5758 mL 2.8788 mL 5.7575 mL 14.3939 mL
10 mM 0.2879 mL 1.4394 mL 2.8788 mL 7.1969 mL
15 mM 0.1919 mL 0.9596 mL 1.9192 mL 4.7980 mL
20 mM 0.1439 mL 0.7197 mL 1.4394 mL 3.5985 mL
25 mM 0.1152 mL 0.5758 mL 1.1515 mL 2.8788 mL
30 mM 0.0960 mL 0.4798 mL 0.9596 mL 2.3990 mL
40 mM 0.0720 mL 0.3598 mL 0.7197 mL 1.7992 mL
50 mM 0.0576 mL 0.2879 mL 0.5758 mL 1.4394 mL
60 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1995 mL
80 mM 0.0360 mL 0.1799 mL 0.3598 mL 0.8996 mL
100 mM 0.0288 mL 0.1439 mL 0.2879 mL 0.7197 mL
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MC2590 Related Classifications

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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