2. Cell Cycle/DNA Damage Epigenetics Apoptosis Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. HDAC Apoptosis Bcr-Abl HSP
  4. MRLB-223

MRLB-223 是一种选择性 HDAC1 和 HDAC2 抑制剂，具有抗肿瘤细胞活性。MRLB-223 可诱导组蛋白高乙酰化、内源性凋亡通路激活、肿瘤细胞凋亡 (apoptosis)、Hsp90 高乙酰化以及半胱天冬酶依赖的 Bcr-Abl 降解。MRLB-223 介导不依赖 p53 的肿瘤细胞死亡，其活性会被 Bcl-2 过表达抑制，且可杀伤表达 Bcr-Abl 的髓系细胞。MRLB-223 可在荷 Eμ-myc 淋巴瘤的小鼠中发挥作用，用于 Eμ-myc 淋巴瘤的研究。

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MRLB-223

MRLB-223 Chemical Structure

CAS No. : 937727-03-2

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MRLB-223 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Bcr-Abl 亚型特异性产品:

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Abl Bcr-Abl

查看 HSP 亚型特异性产品:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRLB-223 is a preferential HDAC1 and HDAC2 inhibitor with activity against tumor cells.MRLB-223 induces histone hyperacetylation, intrinsic apoptotic pathway activation, tumor cell apoptosis, Hsp90 hyperacetylation, and caspase-dependent Bcr-Abl degradation.MRLB-223 mediates p53-independent tumor cell death, with activity suppressed by Bcl-2 overexpression, and kills Bcr-Abl-expressing myeloid cells.MRLB-223 exerts effects in mice bearing Eμ-myc lymphomas.MRLB-223 can be used for the research of Eμ-myc lymphoma[1].

IC50 & Target

HDAC1

 

HDAC2

 

HSP90

 

体外研究
(In Vitro)

MRLB-223 (0.2-10 μM; 24-48 h) 可通过内在凋亡通路以延迟动力学在 Eμ-myc 淋巴瘤细胞中诱导浓度依赖性凋亡，其 24 小时的 IC70 为 5 μM，48 小时的 IC70 为 0.5 μM[1]。
MRLB-223 (0-12 μM; 24 h) 可不依赖 p53 诱导 Eμ-myc 和 Eμ-myc/p53-/- 淋巴瘤细胞发生浓度依赖性凋亡，而 Bcl-2 的过表达可阻断该凋亡效应[1]。
MRLB-223 (0-30 μM; 24-72 h) 可在 FDCP-1 小鼠髓系细胞中诱导浓度依赖性细胞死亡，且具有延迟动力学特征，需要更长的孵育时间才能达到最大效应[1]。
MRLB-223 (0-26 μM; 72 h) 可诱导 FDCP-1/Bcr-Abl 及 FDCP-1/Bcr-AblT315I 细胞发生浓度依赖性细胞死亡，且该过程具有延迟动力学特征，而 Bcr-Abl 降解是半胱天冬酶介导的细胞凋亡的下游结果[1]。
MRLB-223 (10 μM; 24 h) 可在 FDCP-1/Bcr-Abl 细胞中诱导 Hsp90 的高乙酰化，尽管它对 HDAC6 无活性[1]。
MRLB-223 (0-16 μM; 72 h) 可在 FDCP-1/Bcr-Abl 细胞中诱导浓度依赖性细胞死亡，且敲低 HDAC6 不会增强该凋亡效应[1]。

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

MRLB-223 相关抗体:

Cell Viability Assay[1]

Cell Line: Eμ-myc, Eμ-myc/p53-/-, and Eμ-myc/Bcl-2 lymphoma cells
Concentration: 0-12 μM
Incubation Time: 24 h
Result: Induced concentration-dependent PI uptake in Eμ-myc and Eμ-myc/p53-/- cells, with both cell lines showing similar sensitivity.
Suppressed MRLB-223-mediated tumor cell death was observed when Bcl-2 was overexpressed.

Cell Viability Assay[1]

Cell Line: FDCP-1/Bcr-Abl and FDCP-1/Bcr-Abl(T315I) mouse myeloid cells
Concentration: 0-26 μM (72 h PI uptake assay); 5, 10 μM (48 h Bcr-Abl degradation assay)
Incubation Time: 72 h (PI uptake assay); 48 h (Bcr-Abl degradation assay)
Result: Induced concentration-dependent PI uptake in FDCP-1/Bcr-Abl and FDCP-1/Bcr-Abl(T315I) cells at 72 hours, with both cell lines showing equivalent sensitivity.
Induced Bcr-Abl degradation concomitant with apoptosis in cells treated with 5 or 10 μM for 48 hours.
Suppressed apoptosis and maintained Bcr-Abl expression when co-treated with the caspase inhibitor Q-VD-OPh for 48 hours.
体内研究
(In Vivo)

MRLB-223 (15 mg/kg；腹腔注射) 可在携带 Eμ-myc 淋巴瘤的小鼠中发挥抗瘤活性，将中位生存期延长至 42 天，但与广谱 HDAC 抑制剂相比，其组蛋白高乙酰化和抗肿瘤动力学均存在延迟[1]。

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

Animal Model: C57BL/6 (6- to 8-week-old; injected intravenously with 5×105 Eμ-myc lymphoma cells)[1]
Dosage: 15 mg/kg (therapy studies; in vivo apoptosis assays; FDG-PET analysis)
Administration: i.p.; daily, continuous (therapy studies); single dose (in vivo apoptosis assays; FDG-PET analysis)
Result: Reduced average peripheral white blood cell counts to 23.9×103/μL by day 21 and 33.8×103/μL by day 35 (vehicle controls reached 39.2×103/μL by day 21).
Increased median mouse survival to 42 days (vehicle controls had 33 days).
Induced delayed histone H3 and H4 hyperacetylation in lymphoma cells, with minimal acetylation at 2 hours post-dose and gradual increases over time.
Showed no reduction in lymph node FDG uptake at 4 hours post-dose, but a decrease was observed by 48 hours post-dose.
分子量

449.53

Formula

C23H23N5O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MRLB-223 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

MRLB-223937727-03-2MRLB223MRLB 223HDACApoptosisBcr-AblHSPHistone deacetylasesHeat shock proteinstumor cell apoptosisFDCP-1 mouse myeloid cellsp53histone hyperacetylationHsp90 hyperacetylationEμ-myc lymphomasHDAC1intrinsic apoptotic pathwayHDAC2Inhibitorinhibitorinhibit

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