1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. GJ19

GJ19 是一种 PD-L1 抑制剂,其 IC50 值为 32.06 nM。GJ19 能有效结合人源和鼠源 PD-L1 蛋白,KD 值分别为 171 nM和 290 nM。 GJ19 在 HepG2/hPD-L1 与 Jurkat T/hPD-1 细胞共培养模型中可浓度依赖性促进 HepG2 细胞死亡。GJ19 在 B16-F10 黑色素瘤小鼠模型中表现出显著的肿瘤生长抑制作用。GJ19 可用于肿瘤免疫治疗的相关研究。

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GJ19 Chemical Structure

GJ19 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. GJ19 can effectively bind to human/murine PD-L1 protein with KD values of 171 and 290 nM, respectively. GJ19 concentration-dependently promotes HepG2 cell mortality in a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells. GJ19 effectively suppresses tumor growth in a B16-F10 melanoma mouse model. GJ19 can be used for the study of tumor immunotherapy[1].

体外研究
(In Vitro)

GJ19 (48 h) 在 HTRF 实验中表现出最强的 PD-L1 抑制效果,其 IC50 值为 32.06 nM,优于阳性对照BMS-202 (HY-19745) (IC50 = 62.1 nM)[1]

GJ19 (0.1-10 μM) 能有效结合人源/鼠源 PD-L1 蛋白,KD 值分别为 171 nM 和 290 nM[1]

GJ19 (48 h) 对所测试的肿瘤细胞 (小鼠/人类黑色素瘤细胞系 B16-F10/A375、人类肝癌细胞系 HepG2、人类乳腺癌细胞 MDA-MB-231 以及 Jurkat T 细胞) 基本无细胞毒性,其毒性作用仅在与T细胞共培养时才会显现[1]

GJ19 (12.3-1000 nM, 24 h) 在 HepG2/Jurkat T 细胞共培养系统中呈剂量依赖性显著提高 HepG2 细胞的死亡率,且在 1000 nM 浓度下对 HepG2 细胞的杀伤率高于阳性对照 BMS-202[1]

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

体内研究
(In Vivo)

GJ19 (5-15mg/kg, i.p.) 在 B16-F10 黑色素瘤小鼠模型中显示出强大的抗肿瘤功效,注射 15 mg/kg 时肿瘤生长的抑制率 (TGI)为 56.8%[1]

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

Animal Model: 6-8 weeks male C57BL/6 mice were inoculated with B16-F10 cells into the right armpit (2.5×105)([1])
Dosage: 5, 15 mg/kg
Administration: i.p.
Result: Reduced both the tumor weights without affecting the body weight of mice.
Increased the percentages of CD3+ CD4+ cells (helper T cells) and CD3+ CD8+ cells (activated cytotoxic T cells) in melanoma tumors.
Decreased PD-L1 levels in the tumor.
Showed no abnormalities in the weight of major organs (heart, liver, and kidney).
分子量

628.11

Formula

C32H31ClFNO7S

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 *
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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.

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产品名称:
GJ19
目录号:
HY-174830
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