2284460-01-9

2284460-01-9 structure

Name: MC2590
Chemical Name: MC2590
CAS Number: 2284460-01-9
Molecular Formula: C₂₀H₁₇N₃O₃
Molecular Weight: 347.37
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2023-03-11 07:58:32
Modify Date: 2024-09-23 13:18:17
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 ic50 of 0.098 μM, 0.156 μM, 0.039 μM, 0.015 μM, 0.047 μM, 0.071 μM, respectively. MC2590 also inhibits HDAC isoforms HDAC4 (IC50=2.73 μM), HDAC5 (IC50=1.35 μM), HDAC7 (IC50=2.06 μM), HDAC9 (IC50=2.79 μM), HDAC11 (IC50=3.98 μM). MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction[1].

Name	MC2590

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 ic50 of 0.098 μM, 0.156 μM, 0.039 μM, 0.015 μM, 0.047 μM, 0.071 μM, respectively. MC2590 also inhibits HDAC isoforms HDAC4 (IC50=2.73 μM), HDAC5 (IC50=1.35 μM), HDAC7 (IC50=2.06 μM), HDAC9 (IC50=2.79 μM), HDAC11 (IC50=3.98 μM). MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction[1].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC Signaling Pathways >> Epigenetics >> HDAC
Target	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 (化合物5e; 72 小时) 抑制结直肠癌HCT116 (IC50=0.07 μM)、肺腺癌A549 (IC50=0.32 μM)、慢性粒细胞白血病K562 (IC50=0.05 μM)[1]。 MC2625 (1, 5 μM; 24, 48 小时) 诱导 G2/M 细胞周期停滞[1]。 MC2625 (1, 5 μM; 24, 48 小时) 诱导 H3K9/14 过度乙酰化活性，增加乙酰-α-微管蛋白水平，显着上调 p21 蛋白[1]。 MC2625 (1, 5 μM; 48 小时) 增加 p21、BAX 和 BAK 的 mRNA 表达，下调细胞周期蛋白 D1 和 BCL-2，并调节促凋亡和抗凋亡 microRNA 以诱导细胞凋亡[1]。 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).
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.

Molecular Formula	C₂₀H₁₇N₃O₃
Molecular Weight	347.37

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