2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease PI3K/Akt/mTOR MAPK/ERK Pathway GPCR/G Protein Stem Cell/Wnt
  3. Src Cathepsin PI3K Akt Ras Raf ERK MMP
  4. BJ-2302

BJ-2302 是一种 Src 激酶和组织蛋白酶 S (CTSS) 抑制剂，其 IC50 分别为 3.23 和 5.1 μM。BJ-2302 可抑制 PI3K/AKT 和 Ras/Raf/ERK 通路，并降低 CTSS 和 MMP-9 的表达。BJ-2302 可抑制癌细胞的侵袭、转移、增殖以及肿瘤生长。BJ-2302 可用于三阴性乳腺癌的相关研究。

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BJ-2302

BJ-2302 Chemical Structure

CAS No. : 1631056-29-5

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BJ-2302 相关抗体

Top Publications Citing Use of Products

查看 Src 亚型特异性产品:

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Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

查看 Cathepsin 亚型特异性产品:

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Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

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K-Ras H-Ras N-Ras Ras

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B-Raf C-Raf Raf

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

查看 MMP 亚型特异性产品:

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BJ-2302 is a Src kinase inhibitor with an IC50 of 3.23 μM, and inhibits cathepsin S (CTSS) activity[1][2].BJ-2302 binds to Src, suppresses PI3K/AKT and Ras/Raf/ERK pathways, and reduces CTSS and MMP-9 expression[2][3].BJ-2302 inhibits cancer cell invasion, metastasis, proliferation, and tumor growth[1][2][3].BJ-2302 does not induce cytotoxicity in normal breast epithelial cells[3].BJ-2302 can be used for the research of breast cancer and triple-negative breast cancer[1][2][3].

体外研究
(In Vitro)

BJ-2302 可抑制 MDA-MB-231 细胞中 Src 调控的 PI3K/AKT 和 Ras/Raf/ERK 信号通路，抑制 MDA-MB-231 细胞侵袭[1]。
BJ-2302 (0.01-10 µM; 18 h) 可抑制血清诱导的 MDA-MB-231 三阴性乳腺癌 (TNBC) 细胞侵袭，其 IC50 为 0.08 µM、IC90 为 0.71 µM[3]。
BJ-2302 (0.01-10 µM) 以浓度依赖的方式下调 MDA-MB-231 三阴性乳腺癌 (TNBC) 细胞中基础 CTSS 和 MMP-9 的 mRNA 及蛋白表达[3]。
BJ-2302 (0.01-1 µM) 可抑制 NF-κB 的核转位，并以浓度依赖的方式在体外 MDA-MB-231 三阴性乳腺癌 (TNBC) 细胞中抑制 PI3K/Akt 的磷酸化以及 Ras/Raf/ERK 通路分子的磷酸化[3]。
BJ-2302 (0.01-10 µM; 73 h) 以浓度依赖的方式抑制血清诱导的 MDA-MB-231 三阴性乳腺癌 (TNBC) 细胞增殖，在 1 µM 浓度下可完全抑制增殖[3]。
BJ-2302 (0.01-1 µM; 19-73 h) 可在体外以浓度依赖的方式抑制 MDA-MB-231 三阴性乳腺癌 (TNBC) 细胞中 5-羟色胺 (5-HT) 诱导的增殖、侵袭、CTSS/MMP-9 表达以及 Src 磷酸化[3]。

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

BJ-2302 相关抗体:

Cell Invasion Assay[3]

Cell Line: MDA-MB-231 human triple-negative breast cancer (TNBC) cells
Concentration: 0.01, 0.1, 1 and 10 µM
Incubation Time: 18 h
Result: Inhibited serum-induced MDA-MB-231 cell invasion in a concentration-dependent manner, with an IC50 of 0.08 µM and an IC90 of 0.71 µM.
Demonstrated stronger maximum inhibitory effect than Z-FL-COCHO or batimastat, which had IC90 values greater than 10 µM.

Cell Proliferation Assay[3]

Cell Line: MDA-MB-231 human TNBC cells
Concentration: 0.01, 0.1, 1 and 10 µM
Incubation Time: 1 h pre-incubation, then 72 h incubation with serum
Result: Inhibited serum-induced MDA-MB-231 cell proliferation in a concentration-dependent manner.
Achieved complete suppression of serum-induced cell proliferation at 1 µM.
体内研究
(In Vivo)

BJ-2302 (1 mg/kg；腹腔注射；每日 1 次；持续 25 天) 对 BALB/C 裸鼠的三阴性乳腺肿瘤生长具有显著抑制作用，且不会导致进行性体重下降[3]。
BJ-2302 (3-30 pmol/CAM；细胞接种时给药；持续 5 天) 在鸡胚绒毛尿囊膜 (CAM) 异种移植模型中可浓度依赖性地抑制三阴性乳腺癌的肿瘤生长、血管生成及转移[3]。

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

Animal Model: BALB/C nude (7-8 weeks old, female, triple-negative breast cancer subcutaneous model)[3]
Dosage: 1 mg/kg
Administration: i.p.; daily; 25 days
Result: Significantly suppressed tumor volume and tumor weight, with greater efficacy than Z-FL-COCHO (HY-15533) (1 mg/kg) or Batimastat (HY-13564) (30 mg/kg).
Reduced in vivo bioluminescent imaging signals from tumors much lower compared to controls and other treatment groups.
Did not cause progressive body weight loss.
Animal Model: Fertile chicken embryos (developing, triple-negative breast cancer CAM xenograft model)[3]
Dosage: 3 pmol/CAM; 30 pmol/CAM
Administration: at cell inoculation; maintained for 5 days
Result: Suppressed tumor growth and tumor-induced angiogenesis in a concentration-dependent manner, with greater efficacy than Z-FL-COCHO (30 pmol/CAM) or Batimastat (300 pmol/CAM).
Significantly suppressed metastasis of MDA-MB-231-luc2-tdTomato cells to the lungs, liver, and bottom CAM, as evidenced by reduced red-fluorescence-labeled cancer cells and decreased human HPRT mRNA expression in these tissues, with stronger activity than Z-FL-COCHO or batimastat.
分子量

178.19

Formula

C9H10N2O2
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

BJ-2302 相关分类

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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:

BJ-23021631056-29-5BJ2302BJ 2302SrcCathepsinPI3KAktRasRafERKMMPPhosphoinositide 3-kinasePKBProtein kinase BRaf kinasesExtracellular signal regulated kinasesMatrix metalloproteinasescathepsin Striple-negative breast cancerNF-κBPI3K/AKT pathwayMCF-10A cellsMMP-9Src kinaseMDA-MB-231 cellsbreast cancerRas/Raf/ERK pathwayInhibitorinhibitorinhibit

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