2. Epigenetics Apoptosis Cell Cycle/DNA Damage Cytoskeleton
  3. Epigenetic Reader Domain c-Myc Bcl-2 Family PAK Apoptosis
  4. BRD4-IN-12

BRD4-IN-12 是一种强效且口服有效的 BRD4 抑制剂，IC50 为 7.9 nM。BRD4-IN-12 可下调 c-MYC、BCL-2 和 CDK4，并上调 p21。BRD4-IN-12 可抑制肿瘤细胞增殖并促进其凋亡 (apoptosis)。BRD4-IN-12 在 HCT-116 结直肠癌异种移植模型中表现出优异的抗肿瘤效果。BRD4-IN-12 可用于结直肠癌 (CRC) 的研究。

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BRD4-IN-12

BRD4-IN-12 Chemical Structure

CAS No. : 3112325-99-9

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BRD4-IN-12 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC)[1].

IC50 & Target

BRD4

7.90 nM (IC50)

CDK4

 

Bcl-2

 

体外研究
(In Vitro)

BRD4-IN-12 (H5) (72 h) 对 HCT-116 结直肠癌细胞表现出细胞毒性，IC50 值为 0.84 μM，且 BRD4-IN-12 在 HCT-116 细胞中诱导的细胞毒性依赖于 BRD4[1]。
BRD4-IN-12 (1.25-5.0 μM; 24 h) 可下调 HCT-116 细胞中 c-MYC、CDK4 和 BCL-2 的蛋白表达，并呈剂量依赖性地上调 p21 的蛋白表达[1]。
BRD4-IN-12 (20 μM；3 h) 可稳定 HCT-116 细胞裂解液中的 BRD4 蛋白，证实其与 BRD4 存在细胞内结合[1]。

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

BRD4-IN-12 相关抗体:

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 1.25 μM, 2.5 μM, 5.0 μM
Incubation Time: 24 h
Result: Downregulated the expression of c-MYC, CDK4 and BCL-2 proteins; upregulated p21 levels in a dose-dependent manner.

Cell Viability Assay[1]

Cell Line: HCT-116 cells
Concentration: 10 μM
Incubation Time: 72 h
Result: 10 μM concentration showed 92% inhibition rate against HCT-116 cells.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-inf CL Vz F
Mice[1] 2 mg/kg i.v. 0.29 h - h - ng/mL 456 ng·h/mL 458 ng·h/mL 73.8 mL/min/kg 1.20 L/kg - %
Mice[1] 25 mg/kg p.o. 1.49 h 0.333 h 81.3 ng/mL 86.0 ng·h/mL 95.9 ng·h/mL - mL/min/kg - L/kg 1.51 %
体内研究
(In Vivo)

BRD4-IN-12 (H5) (25 mg/kg or 50 mg/kg; 口服；每日一次；持续 18 天) 在荷 HCT-116 结直肠癌异种移植瘤的雄性 BALB/c 裸鼠中，分别以 25 mg/kg 和 50 mg/kg 的剂量表现出 52% 和 82% 的肿瘤生长抑制率 (TGI)；维持体重稳定，且未对主要器官 (心脏、肝脏、脾脏、肺、肾脏) 造成显著的病理损伤；并下调肿瘤组织中 c-MYC 和 BCL-2 的表达；诱导肿瘤组织中细胞间距增大、细胞核变小变圆[1]。

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

Animal Model: Male BALB/c nude mice (4-6 weeks old, 18-22 g) were subcutaneously inoculated with HCT-116 cells (5 × 106 cells/mL)[1].
Dosage: 25 mg/kg or 50 mg/kg
Administration: dissolved in vehicle containing 5% ethanol, 40% PEG 400, 5% Tween 80, and 50% water; Oral (p.o.) administration; once daily; for 18 days
Result: Both doses maintained stable body weight and caused no obvious pathological damage to major organs (heart, liver, spleen, lung, kidney).
Both doses downregulated the expression of c-MYC and BCL-2 in tumor tissues and induced increased cell spacing, smaller and rounded nuclei in tumor tissues (H&E staining).
The 25 mg/kg dose exhibited 52 % tumor growth inhibition (TGI) without significant body weight loss.
The 50 mg/kg dose achieved 82 % tumor growth inhibition (TGI) and downregulated the expression of c-MYC and BCL-2 in tumor tissues.
分子量

428.50

Formula

C21H24N4O4S
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

BRD4-IN-12 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

BRD4-IN-123112325-99-9Epigenetic Reader Domainc-MycBcl-2 FamilyPAKApoptosisMycp21 activated kinasesBRD4 inhibitorantitumor efficacydownregulates c-MYC/BCL-2/CDK4upregulates p21HCT-116 cellsBALB/c nude miceHCT-116 xenograft modelcolorectal cancer (CRC)Inhibitorinhibitorinhibit

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