1. Anti-infection Cell Cycle/DNA Damage
  2. Bacterial DNA/RNA Synthesis
  3. GKL003

GKL003 是一种靶向 RNAP-σ 相互作用界面的细菌转录抑制剂,其 Ki 为 5.79 nM。GKL003 特异性结合于 σA 因子作用位点处的 RNAP β' 钳状螺旋区域,阻断 RNAP 全酶的形成,并抑制细菌转录起始复合物的形成。GKL003 可抑制革兰氏阳性菌和革兰氏阴性菌细胞的生长,且对耐药菌株也具有活性。

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GKL003

GKL003 Chemical Structure

CAS No. : 1445801-61-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GKL003 is a bacterial transcription inhibitor that targets the RNAP-σ interaction interface, with a Ki of 5.79 nM. GKL003 specifically binds to the RNAP β' clamp helix region at the σA factor binding site, blocks the formation of RNAP holoenzyme, and inhibits the formation of bacterial transcription initiation complexes. GKL003 inhibits the growth of both Gram-positive and Gram-negative bacterial cells, and also exhibits activity against drug-resistant strains[1].

体外研究
(In Vitro)

GKL003 (0.5-25 μM) 可抑制大肠杆菌 RNAP 核心酶与枯草芽孢杆菌 σᴬ 的体外转录,在 σᴬ:RNAP 核心酶的亚饱和比例 0.5:1 时观察到更强的抑制作用[1]
GKL003 (0-500 nM) 可抑制大肠杆菌 RNAP 核心酶与枯草芽孢杆菌 σᴬ 的体外转录活性,其抑制常数 Ki 为 5.79 nM[1]
GKL003 (10-500 nM) 可抑制大肠杆菌 RNAP 核心酶与大肠杆菌 σ70 的体外转录活性[1]

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

体内研究
(In Vivo)

GKL003 (1-2 mM) 可在 ≥1 mM 浓度下显著抑制革兰氏阴性 E. coli DH5α 培养物的生长[1]
GKL003 (0.5-2 mM) ≥ 1 mM 时显著抑制革兰氏阳性耐 Methicillin (HY-121544) 金黄色葡萄球菌USA300 菌株的生长,并可剂量依赖性地抑制活金黄色葡萄球菌 USA300 细胞的转录[1]

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

分子量

659.52

Formula

C34H28Cl2N4O6

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

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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.

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GKL003
目录号:
HY-102072
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