2. Metabolic Enzyme/Protease
  3. Heme Oxygenase (HO)
  4. KCL-HO-1i

KCL-HO-1i 是一种口服活性的 heme oxygenase-1 (HO-1) 抑制剂 (大鼠 HO-1: IC50 = 123 nM，人 HO-1: IC50 = 128 nM)。KCL-HO-1i 针对肿瘤微环境 (TME) 中免疫抑制的 LYVE-1+ 血管周肿瘤相关巨噬细胞 (PvTAMs)，减少 PvTAM 介导的免疫排斥。KCL-HO-1i 在 MMTV-PyMT 自发性乳腺癌小鼠或携带皮下 MN-MCA1 肉瘤的 C57Bl/6 小鼠中与化疗显示出协同抗肿瘤效果。KCL-HO-1i 可用于癌症研究。

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KCL-HO-1i

KCL-HO-1i Chemical Structure

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KCL-HO-1i 相关抗体

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查看 Heme Oxygenase (HO) 亚型特异性产品:

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HO-1 HO-2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KCL-HO-1i is an orally active heme oxygenase-1 (HO-1) inhibitor (rat HO-1: IC50 = 123 nM) and human HO-1: IC50 = 128 nM). KCL-HO-1i targets immunosuppressive LYVE-1+ perivascular tumor-associated macrophages (PvTAMs) in the tumor microenvironment (TME), reduces PvTAM-mediated immune exclusion. KCL-HO-1i demonstrates synergistic anti-tumor efficacy with chemotherapy in MMTV-PyMT spontaneous breast cancer mice or C57Bl/6 mice bearing subcutaneous MN-MCA1 sarcomas. KCL-HO-1i can be used for the study of cancer[1].

IC50 & Target[1]

HO-1

123 nM (IC50, rat splenic microsomes )

HO-1

128 nM (IC50, HEK293T cells )

体外研究
(In Vitro)

KCL-HO-1i 对大鼠脾微粒体中的大鼠 heme oxygenase-1 (HO-1) (IC50 = 123 nM) 和 HEK293T 细胞 (IC50 = 128 nM) 表现出抑制活性[1].
KCL-HO-1i (25 μM, 16 h) 改善 CD8+ T 细胞的跨内皮迁移，逆转了在 transwell 实验中由 IL-6 极化的骨髓源性巨噬细胞引起的迁移限制[1].

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

KCL-HO-1i 相关抗体:
体内研究
(In Vivo)

KCL-HO-1i (27.8 mg/kg (25 μMol/kg)，口服，每日一次，21 天) 单独使用可减缓肿瘤生长，并与化疗 (5-fluorouracil (HY-90006) 或 Gemcitabine (HY-17026)) 协同作用，在 MMTV-PyMT 自发性乳腺癌小鼠和携带皮下 MN-MCA1 肉瘤的 C57Bl/6 小鼠中实现持久的肿瘤生长控制[1].

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

Animal Model: Transgenic MMTV-PyMT mice (FVB/N background) with spontaneous breast tumor development or MN-MCA1 sarcoma cells (2.5 × 105 in 100 µL RPMI 1640) were subcutaneously implanted into the flanks of 21-25 g female C57Bl/6 mice to establish ectopic sarcoma tumorsMN-MCA1 sarcoma cells (2.5 × 10⁵ in 100 µL RPMI 1640) were subcutaneously implanted into the flanks of 21-25 g female C57Bl/6 mice to establish ectopic sarcoma tumors[1]
Dosage: p.o., daily, 21 days
Administration: 25 μMol/kg, alone or combined with chemotherapy (5-fluorouracil (40 mg/kg/4 days) or Gemcitabine (6.6 mg/kg/7 days)
Result: Achieved tumor growth control.
Caused mild pulmonary inflammation (grade 2-3) in mice.
Reduced the expression of TIM3 (an inhibitory immune checkpoint receptor) on CD8+ T-cells.
分子量

1110.75

Formula

C34H36N4O12P2Sn3
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

KCL-HO-1i 相关分类

  • 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.

Keywords:

KCL-HO-1iHeme Oxygenase (HO)Heme OxygenasecancerMMTV-PyMT spontaneous breast cancerMN-MCA1 sarcomasHO-1Inhibitorinhibitorinhibit

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