2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Pyruvate Kinase Interleukin Related
  4. LIQ1

LIQ1 是一种黄酮类衍生物，是一种强效的丙酮酸激酶 M2 (PKM2) 变构抑制剂 (IC50 = 0.39 μM；Kd = 4.5 μM)，靶向多聚精氨酸口袋中的 Arg43。LIQ1 在 LPS (HY-D1056) 诱导的小鼠内毒素血症模型中显示出药效，可阻止 PKM2 的核转位并抑制其与 HIF-1α 的结合，从而抑制 IL-1β 的转录。LIQ1 可用于内毒素血症的研究。

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LIQ1

LIQ1 Chemical Structure

CAS No. : 2606032-80-6

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LIQ1 相关抗体

Top Publications Citing Use of Products

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LIQ1, a flavonoid derivative, is a potent Pyruvate kinase M2 (PKM2) allosteric inhibitor (IC50 = 0.39 μM; Kd = 4.5 μM) targeting Arg43 within the polyarginine pocket. LIQ1 exhibits efficacy in a mouse model of LPS (HY-D1056)-induced endotoxemia, preventing the nuclear translocation of PKM2 and inhibiting its binding to HIF-1α, thereby suppressing IL-1β transcription. LIQ1 can be used for the research of endotoxemia[1].

IC50 & Target[1]

PKM2

0.39 μM (IC50)

PKM2

4.5 μM (Kd)

体外研究
(In Vitro)

LIQ1 (100 μM；2 小时) 显著增强了 PKM2 在 40-52 ℃ 温度范围内的热稳定性，使其熔解温度 (Tm) 升高了 3.4 ℃[1]。
与野生型 PKM2 (IC50 = 0.98 μM; Kd = 3.2 μM) 相比，LIQ1 显著降低了对 PKM2 R43A (IC50 = 4.10 μM; Kd = 11.1 μM) 的抑制作用，表明 R43 是介导 PKM2 变构抑制的关键残基[1]。

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

LIQ1 相关抗体:
体内研究
(In Vivo)

LIQ1 (1、2 和 5 mg/kg；腹腔注射；在 LPS 注射后 0、12、24 和 36 小时给药) 显著改善了 LPS 诱导的小鼠内毒素血症的存活率，并减少了炎症和器官损伤[1]。
LIQ1 (20 mg/kg；腹腔注射；单次给药；或每日一次，连续 14 天) 在小鼠中显示出可忽略的急性毒性和无肝肾毒性，支持其良好的安全性[1]。

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

Animal Model: Male BALB/c mice (6-8 weeks old) intraperitoneally injected with LPS (13 mg/kg)[1]
Dosage: 1, 2, 5 mg/kg
Administration: i.p.; administered at 0, 12, 24, and 36 h after LPS injection
Result: Increased the 7-day survival rate from 40% (1 mg/kg) to 80% (5 mg/kg).
Exhibited a dose-dependent reduction in serum IL-1β levels.
Mitigated the injuries induced by LPS, such as microvilli loss, villus atrophy, deformation, and necrosis.
Alleviated the LPS-induced pathological lesions in the lung and heart tissues at the dose of 5 mg/kg.
Suppressed LPS-induced ATP accumulation.
Significantly inhibited the nuclear translocation of PKM2 in the small intestine, lung, and heart tissues.
Prevented PKM2-HIF-1α complex formation, ultimately leading to reduced IL-1β transcription in mice.
Animal Model: Male BALB/c mice (6-8 weeks old)[1]
Dosage: 20 mg/kg
Administration: i.p.; single dose
Result: Showed no significant decrease in body weight over 14 days.
Revealed no changes in motor activity, grooming and rubbing behaviors.
Animal Model: Male BALB/c mice (6-8 weeks old)[1]
Dosage: 20 mg/kg
Administration: i.p.; daily for 14 days
Result: Revealed a significant increase in alkaline phosphatase (ALP) levels.
Showed no statistically significant changes in other liver enzymes, including AST, ALT, GGT, total protein (TP), albumin (ALB), and globulin (GLO).
Showed no significant effects on kidney function parameters, including urea, creatinine (CREA), uric acid (UA), and estimated glomerular filtration rate (eGFR).
分子量

284.26

Formula

C16H12O5
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

LIQ1 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:

LIQ12606032-80-6LIQ 1LIQ-1Pyruvate KinaseInterleukin RelatedILAllosteric inhibitorPyruvate kinase M2Polyarginine pocketInhibitorinhibitorinhibit

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目录号：
HY-179371
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