2. Apoptosis Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Apoptosis Caspase HSP Early 2 Factor (E2F) DNA/RNA Synthesis
  4. Ly101-4B

Ly101-4B 是一种凋亡 (apoptosis) 诱导剂和多靶点抑制剂，具有抗增殖、抗肿瘤与细胞毒性效应。Ly101-4B 可降低 HSF1 表达、抑制 microRNA-214 合成，并下调 HSP27、HSP70、HSP90 表达，同时抑制 E2F 依赖性转录活性并下调其靶基因。Ly101-4B 通过减少 DNA 合成、抑制细胞周期与 G1/S 期转换等方式诱导 caspase 3/7 介导的凋亡，不影响 RNA 合成或引发坏死。Ly101-4B 对不同基因型及 E2F 依赖程度的胰腺导管腺癌细胞具有选择性。Ly101-4B 可用于上皮性卵巢癌和胰腺导管腺癌的相关研究。

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Ly101-4B

Ly101-4B Chemical Structure

CAS No. : 1415728-94-7

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Ly101-4B 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ly101-4B is an apoptosis inducer and multi-target inhibitor with antiproliferative, antitumor and cycytotoxic effects. Ly101-4B reduces HSF1 expression, inhibits microRNA-214 synthesis, downregulates HSP27, HSP70 and HSP90 expression, while suppressing E2F-dependent transcriptional activity and downregulating its target genes. Ly101-4B induces caspase 3/7-mediated apoptosis by reducing DNA synthesis, inhibiting the cell cycle and G1/S phase transition, without affecting RNA synthesis or inducing necrosis. Ly101-4B is selective for pancreatic ductal adenocarcinoma cells with different genotypes and varying degrees of E2F dependence. Ly101-4B can be used in research related to epithelial ovarian cancer and pancreatic ductal adenocarcinoma[1][2][3].
IC50 & Target

Caspase-3

 

Caspase-7

 

HSP70

 

HSP90

 

HSF1

 

体外研究
(In Vitro)

Ly101-4B (20-100 μM；24-48 h) 可抑制人上皮性顺铂耐药卵巢癌细胞 SKOV3 的增殖、诱导其凋亡，并下调该细胞中 HSF1、HSP27、HSP70 和 HSP90 的表达[1]。
Ly101-4b (20-100 μM；48 小时) 可降低原代 Nupr1 缺陷型和 Nupr1 wt；KIC 胰腺癌细胞的活力，在 100 μM 浓度下存在显著的差异效应[2]。
Ly101-4B (1-25 μM；12-72 h) 在E2F 依赖性报告基因载体的荧光素酶活性验证实验中，可抑制 MiaPaCa2 细胞中的 E2F 活性[3]。
Ly101-4B (25 μM；12-72 h) 可降低 MiaPaCa2 细胞的活力，诱导 caspase 3/7 介导的细胞凋亡，并抑制 DNA 合成，但不影响 RNA 合成或引发细胞坏死[3]。
Ly101-4B 对 E2F 高表达原代 PDAC 细胞 (CRCM93、CRCM08、CRCM17) 的效力优于 E2F 低表达原代 PDAC 细胞 (CRCM10、CRCM12、CRCM110、CRCM92)，其 72 h IC50值更低 (19.4 μM vs 44.1 μM)[3]。

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

Ly101-4B 相关抗体:

Cell Proliferation Assay[1]

Cell Line: SKOV3 human epithelial cisplatin-resistant ovarian cancer cells
Concentration: 60 μM (HSF1 protein depletion); 20-100 μM (cell viability assessment)
Incubation Time: 48 h (HSF1 protein depletion, cell viability assessment); 24 h (HSF1 mRNA measurement)
Result: Efficiently inhibited cell proliferation with greater efficiency than cisplatin. Decreased HSF1 mRNA levels after 24 h of treatment. Considerably depleted HSF1 protein expression after 48 h of treatment. Increased the percentage of early apoptotic cells from 5.0% to 19.0%. Accumulated the cleaved form of caspase9 (p35 segment). Considerably decreased protein expression of HSP27, HSP70, and HSP90.

Cell Viability Assay[2]

Cell Line: primary Nupr1-deficient pancreatic cancer cells, primary Nupr1wt;KIC pancreatic cancer cells
Concentration: 20, 50, 100 μM
Incubation Time: 48 h
Result: Induced a reduction in cell viability in both Nupr1-deficient and Nupr1wt; KIC cells starting from 20 μM. Showed activity comparable to that of gemcitabine from 50 μM. Observed a significant differential response at 100 μM.
体内研究
(In Vivo)

Ly101-4B (100 mg/kg；腹腔注射；每周 2 次；持续 4 周) 在雌性裸鼠（无胸腺小鼠）中，可通过下调 HSF1 和 miR-214 显著抑制卵巢肿瘤的体内生长，且无不良反应[1]。

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

Animal Model: BALB/c-nu/nu (female, 4-week old)[1]
Dosage: 100 mg/kg
Administration: i.p.; twice a week; 4 weeks
Result: Significantly retarded tumor growth compared to control;
Detected few Ki-67-positive cells in treated tumors;
Sharply decreased HSF1-positive cells and staining intensity;
Depleted HSF1 mRNA and miR-214 levels in treated tumors.
分子量

442.51

Formula

C23H30N4O5
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

Ly101-4B 相关分类

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  • 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:

Ly101-4B1415728-94-7ApoptosisCaspaseHSPEarly 2 Factor (E2F)DNA/RNA SynthesisHeat shock proteinsepithelial ovarian cancerE2F transcription factor familyapoptosisHSP70HSP27SKOV3 human epithelial cisplatin-resistant ovarian cancer cellsMiaPaCa2 cellsHO8910 human ovarian cancer cellspancreatic ductal adenocarcinoma cellsheat shock factor 1 (HSF1)Inhibitorinhibitorinhibit

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