2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. LGF308

LGF308 是一种 BRD4 的 PROTAC 降解剂，对癌细胞的细胞毒性比对正常细胞具有选择性。LGF308 介导 BRD4 与 DCAF11 形成三元复合物，从而实现 BRD4 降解。LGF308 通过上调凋亡相关蛋白诱导肿瘤细胞凋亡。LGF308 可抑制乳腺癌和三阴性乳腺癌细胞系中的肿瘤细胞增殖和迁移。LGF308 可用于乳腺癌的研究。

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LGF308

LGF308 Chemical Structure

CAS No. : 3061406-69-4

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LGF308 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer[1].

体外研究
(In Vitro)

LGF308 (10 nM-1 μM; 12 h) 可在低至 10 nM 浓度作用 12 h 的条件下，强效诱导 BD1-HEK293T 报告细胞中的 BD1 降解[1]。
LGF308 (0.1-5 μM; 3-9 h) 可在 MDA-MB-231 细胞中诱导 BRD4 发生时间和浓度依赖性降解，其长亚型的 DC50 值为 0.50 μM，短亚型的 DC50 值为 0.23 μM；在 5 μM 作用 9 h 时，降解率可达 >90%[1]。
LGF308 (1 μM) 在 MDA-MB-231 细胞中诱导的 BRD4 降解依赖于泛素-蛋白酶体途径，而非溶酶体途径[1]。
LGF308 (0.1-10 μM; 12 h) 可在 BD1-HEK293T 细胞和 CRISPRi HEK293T 细胞中诱导依赖于 DCAF11 的 BRD4/BD1 降解[1]。
LGF308 (1 μM; 6 h) 可在 HEK293T 细胞中促进 BD1 与 DCAF11 形成三元复合物[1]。
LGF308 (gradient concentrations; 48 h) 可选择性抑制乳腺癌细胞系的增殖，在 MDA-MB-468 细胞中活性最强 (IC50 = 0.70 μM)，而在正常 HEK293T 细胞中活性较低 (IC50 = 16.01 μM)[1]。
LGF308 (1 μM) 可诱导 MDA-MB-231 细胞发生细胞凋亡，这一点可通过 c-PARP-1 和 c-Caspase-7 表达水平上调得到证实[1]。

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

LGF308 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2 μM, 5 μM (9 h treatment); 1 μM (3 h, 6 h, 9 h treatments)
Incubation Time: 3 h, 6 h, 9 h (1 μM treatment); 9 h (0.1-5 μM treatments)
Result: Reduced BRD4 levels to ~60% of control after 3 h of 1 μM treatment.
Dropped BRD4 levels to ~40% of control by 6 h of 1 μM treatment.
Degraded over 90% of both long and short BRD4 isoforms at 5 μM, with a DC50 of 0.50 μM for the long isoform and 0.23 μM for the short isoform.

Cell Proliferation Assay[1]

Cell Line: MCF-7, T-47D, MDA-MB-231, MDA-MB-157, MDA-MB-468, HCC1937, BT-549 (breast cancer cell lines), HEK293T (normal cell line)
Concentration: Gradient concentrations
Incubation Time: 48 h
Result: Inhibited proliferation of breast cancer cell lines with IC50 values of 2.86 μM (MCF-7), 2.22 μM (T-47D), 1.31 μM (MDA-MB-231), 3.10 μM (MDA-MB-157), 0.70 μM (MDA-MB-468), 1.45 μM (HCC1937), 1.60 μM (BT-549).
Resulted in an IC50 of 16.01 μM for normal HEK293T cells, significantly higher than cancer cell lines.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Vdss MRT0-inf CL Cmax AUC0-t AUC0-∞
Rat[1] 3 mg/kg i.v. 3.84 h 0.08 L/kg 1.72 h 0.73 mL/min/kg 30,833.3 ng/mL 114,985 115,124
分子量

732.27

Formula

C35H34ClN7O5S2
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

LGF308 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

LGF3083061406-69-4LGF 308LGF-308PROTACsEpigenetic Reader DomainHEK293T cellsMDA-MB-468 cellsbreast cancerDCAF11triple-negative breast cancerE3 ligaseMDA-MB-231 cellsproteasomal pathwayBRD4apoptosisInhibitorinhibitorinhibit

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