1. Epigenetics Immunology/Inflammation JAK/STAT Signaling Stem Cell/Wnt
  2. Epigenetic Reader Domain Interleukin Related STAT
  3. KB-0118

KB-0118 (BBC0115) 是 BET 溴结构域抑制剂。KB-0118 选择性结合 BRD2 和 BRD4,而非 BRD3,其 Kd 值对 BRD2 BD1 为 36.7 μM,对 BRD4 BD1 为 47.4 μM。KB-0118 抑制促炎细胞因子的分泌,包括 TNFIL-1βIL-23a,并选择性抑制 Th17 细胞分化。KB-0118 通过 BRD4 的表观遗传抑制来调节 Th17 驱动的炎症,这通过 STAT3 和 BRD4 靶基因的下调得到证实。KB-0118 在炎症性肠病 (IBD) 模型中具有免疫调节作用[1]

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

KB-0118 Chemical Structure

KB-0118 Chemical Structure

CAS No. : 2648377-08-4

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KB-0118 (BBC0115) is BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model[1].

IC50 & Target[1]

BRD2 BD1

36.7 μM (Kd)

BRD2 BD2

74.3 μM (Kd)

BRD4 BD1

47.4 μM (Kd)

BRD4 BD2

41.7 μM (Kd)

STAT3

 

IL-1β

 

IL-23a

 

体外研究
(In Vitro)

KB-0118 (1-10 μM,12 小时) 可下调经 PMA (HY-18739)/Lonomycin (HY-122466) 处理的 Jurkat 细胞中的促炎细胞因子 (例如:TNF、MIF 和 CSF2)[1]


KB-0118 (1-10 μM,12 小时) 可下调经 LPS (HY-D1056) 处理的 RAW 264.7 细胞中的促炎细胞因子 (例如:IL-1β、IL-6、IL-23a 和 Cxcl11)[1]


KB-0118 (5 μM,5 天) 可抑制抗 CD3 和抗 CD28 激活的小鼠 CD4+ T 细胞增殖,其表现为分裂、增殖、扩增和复制指数下降[1]


KB-0118 (5 μM,5天) 降低 Th17 细胞 (RORγt+ IL-17A+) 的比例,表明其抑制了 Th17 细胞的分化[1]


KB-0118 (5 μM,5天) 增加 Th2 细胞 (GATA-3+ IL-4+) 的比例,表明其促进了 Th2 细胞的极化[1]


KB-0118 (0.01-1 μM,24小时) 提高了经 DSS (5%,48小时) 处理的 Caco-2 细胞的细胞活力[1]

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

RT-PCR[1]

Cell Line: Jurkat cells
Concentration: 1 μM, 5 μM, 10 μM
Incubation Time: Pretreated for 6 h and then co-incubated with PMA/Lonomycin for 6 h
Result: Downregulated pro-inflammatory cytokines, particularly TNF, MIF, and CSF2, TGFB1, and these reductions were statistically significant at 5 μM and 10 μM.
Upregulated IL-3, IL-4, and IL-26.
体内研究
(In Vivo)

KB-0118 (200 mg/kg,溶于饮用水,7 天) 可缓解 DSS (HY-116282C) (3% 溶于饮用水) 诱发的结肠炎模型中的结肠炎[1]


KB-0118 (50 mg/kg,口服,每日一次,疗程6周) 可通过降低慢性T细胞介导结肠炎模型中 IL-17a 驱动的炎症来缓解T细胞介导的结肠炎[1]


KB-0118 (50-250 mg/kg,灌胃14 天)在雄性和雌性C57BL/6小鼠中均表现出良好的耐受性[1]

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

Animal Model: DSS (HY-116282C) (3 % in drinking water)-induced colitis model in male C57BL/6 mice[1].
Dosage: 200 mg/kg
Administration: In drinking water, for 7days
Result: Had a significant protective effect on colon length, preserving colon integrity and reducing inflammation compared to the DSS-only group.
Reduced epithelial damage and immune cell infiltration compared to DSS-only mice.
Provided a slight, non-significant reduction in weight loss and the Disease Activity Index (DAI) compared to DSS-only mice.
Animal Model: A chronic colitis model induced by adoptive transfer of CD45RBhigh T cells into RAG1 KO mice[1].
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.), daily for 6 weeks
Result: Attenuated weight loss and increased colon length compared to vehicle-treated controls.
Reduced epithelial damage and immune cell infiltration in the colon, showing greater efficacy than MS402 (HY-120000).
Reduced IL-17a levels in the DSS-treated colons.
Down-regulated critical genes for T cell activation and cytotoxicity, such as Cd3e, Lck, and Stat4, as well as integrin genes like Itgam and Itgal (bulk RNA sequencing).
Reduced expression of genes regulated by immune-related TFs, such as IRF8, FOXO1, and RUNX1 (bulk RNA sequencing).
分子量

309.27

同用名

BBC0115

Formula

C17H11NO5

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
  • 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.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
KB-0118
目录号:
HY-176535
需求量: