2. Epigenetics
  3. Histone Methyltransferase
  4. BBDDL2059

BBDDL2059 是一种选择性组蛋白甲基转移酶 EZH2 共价抑制剂，对于 EZH2-Y641F 的 IC50 为 1.5 nM。BBDDL2059 在纳摩尔浓度下抑制淋巴瘤细胞生长，可用于抗癌研究。

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BBDDL2059 Chemical Structure

BBDDL2059 Chemical Structure

CAS No. : 2691174-27-1

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BBDDL2059 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research[1].

IC50 & Target[1]

EZH2 Y641F mutant type

1.5 nM (IC50)

体外研究
(In Vitro)

BBDDL2059 (Compound 16) (0-65 nM；6 天) 抑制 KARPAS-422 和 Pfeiffer 细胞生长[1]。
BBDDL2059 (0-1 μM；48-96 小时) 抑制 EZH2 酶活性，并在清洗后维持对 EZH2 的长期抑制[1]。

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

BBDDL2059 相关抗体:

Cell Proliferation Assay[1]

Cell Line: KARPAS-422 cells and Pfeiffer cells
Concentration: 0-65 nM
Incubation Time: 6 day
Result: Inhibited cell growth with IC50s of 64 nM and 22 nM for KARPAS-422 and Pfeiffer cells, respectively.

Western Blot Analysis[1]

Cell Line: KARPAS-422 cells and Pfeiffer cells
Concentration: 0.05,0.1,0.5,1 μM
Incubation Time: 48-96 hours
Result: Effective reduces H3K27me3 in Pfeiffer cells in a concentration- and time-dependent manner.
Significantly inhibited the levels ofH3K27me3 in cells after treated within 96h after being washed out, and the levels of H3K27me3 were still lower than negative control after 120 h.
体内研究
(In Vivo)

BBDDL2059 (Compound 16) (静脉注射 3 mg/kg，口服 10 mg/kg) 在大鼠中显示 T1/2 为 0.28 小时 (静脉注射)，口服生物利用度 (F%) 为 0.05%[1]。
Pharmacokinetic parameters for BBDDL2059 (Compound 16) in rats[1]

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

Route Dose (mg/kg) T1/2 (h) Cmax (ng/mL) AUC0-last (h•ng/mL) CL (mL•min-1/kg-1) Vss (L/kg) F (%)
iv 3 0.28 / 4886 11.1 161 /
po 10 / 29.5 8.16 / / 0.05
Animal Model: Rats(Pharmacokinetic assay)[1]
Dosage: 3 or 10 mg/kg
Administration: Oral gavage (p.o.), Intravenous injection (i.v.)
Result: Showed a T1/2 of 0.28h (i.v.) and oral bioavailability (F%) of 0.05%.
分子量

512.66

Formula

C27H36N4O4S
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

BBDDL2059 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

BBDDL20592691174-27-1BBDDL 2059BBDDL-2059Histone MethyltransferaseHistone Methyltransferase,EZH2covalent inhibitorcancerKARPAS-422Pfeiffer cellsInhibitorinhibitorinhibit

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目录号：
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