1. Apoptosis Epigenetics Cell Cycle/DNA Damage
  2. Apoptosis PARP
  3. Sino-C

Sino-C 是一种具有抗癌活性的 Sinomenine (HY-15122) 衍生物。Sino-C 通过上调 SREBF2HMGCS1 等关键基因广泛破坏胆固醇稳态,导致细胞内胆固醇积聚和脂滴形成。Sino-C 诱导的代谢紊乱进一步触发脂质过氧化和内质网 (ER) 应激,从而启动一种独特的混合型细胞死亡形式,包括凋亡 (apoptotic) (剪切 PARP) 及坏死样特征。Sino-C 可用于结直肠癌、肺癌、乳腺癌研究。

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Sino-C

Sino-C Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sino-C is a Sinomenine (HY-15122) derivative with anticancer activity. Sino-C broadly disrupts cholesterol homeostasis by upregulating key genes such as SREBF2 and HMGCS1, leading to intracellular cholesterol accumulation and lipid droplet formation. Sino-C-induced metabolic dysregulation further triggers lipid peroxidation and endoplasmic reticulum (ER) stress, initiating a unique form of hybrid cell death including apoptotic (cleaved PARP) and necrotic-like features. Sino-C thus serves as a useful compound for research in colorectal cancer, lung cancer and breast cancer[1].

体外研究
(In Vitro)

Sino-C (0-20 μM,48 小时) 在结直肠癌 (HCT116、RKO 和 MC38)、肺癌 (A549 和 NCI-H1299) 及乳腺癌 (MDA-MB-231 和 4T1) 细胞中表现出广谱抗癌活性[1]
Sino-C (0-20 μM,24 小时) 在 HCT116 和 RKO 细胞中显示出显著的抗结直肠癌效果[1]
Sino-C (0-20 μM,24 小时) 诱导 HCT116 和 RKO 细胞死亡,其特征为 PARP 剪切而无 caspase-3 活化,并引起严重的形态学改变 (核周间隙增宽、内质网显著扩张伴随核糖体脱落、线粒体肿胀),同时伴有明显的乳酸脱氢酶泄漏和细胞膜损伤,提示存在非凋亡性机制[1]
Sino-C (24 h) 引发一种独特的细胞死亡形式:其形态特征不符合经典的凋亡、副凋亡、焦亡或铁死亡,而是呈现出一种结合了凋亡与坏死样特征的混合模式 (在 HCT116 细胞中)[1]
Sino-C (0-20 μM) 在 HCT116 细胞中上调胆固醇稳态相关基因、提高细胞内胆固醇水平并诱导脂滴积累[1]
Sino-C (0-20 μM,24 小时) 诱导胆固醇失调,该作用继而导致脂质过氧化并随后触发内质网应激,最终促成结直肠癌细胞死亡[1]

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

Cell Viability Assay[1]

Cell Line: HCT116, RKO, MC38, A549, NCI-H1299, MDA-MB-231, 4T1
Concentration: 1.25, 2.5, 5, 10 and 20 μM
Incubation Time: 48 h
Result: Significantly reduced cell viability in all tested cell lines in a dose-dependent manner, with IC50 values predominantly below 10 μM.
Showed greater potency against CRC cell lines, with IC50 values of 5.15 μM (HCT116), 9.72 μM (RKO), and 4.58 μM (MC38).

Cell Proliferation Assay[1]

Cell Line: HCT116 and RKO cells
Concentration: 0, 5, 10 and 20 μM
Incubation Time: 24 h
Result: Remarkably inhibited the colony formation of HCT116 and RKO cells.

Apoptosis Analysis[1]

Cell Line: HCT116 and RKO cells
Concentration: 0, 5, 10 and 20 μM
Incubation Time: 24 h
Result: Revealed a dose-dependent increase in apoptosis: from 5.81% (control) to 26.80% (20 μM) in HCT116 cells from 5.39% to 22.34% in RKO cells.
Had minimal Annexin V+ staining in both cell lines, indicating a limited externalization of phosphatidylserine on the plasma membrane.
Increased in PI+ stained cells upon Sino-C treatment, suggesting that apoptosis may not be the only cell death mode.

RT-PCR[1]

Cell Line: HCT116 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Upregulated key genes involved in cholesterol homeostasis, including the master transcriptional Regulator of cholesterol biosynthesis, SREBF2, as well as rate-limiting enzymes and a key Receptor in the pathway, such as HMGCS1, SQLE, and LDLR.

Immunofluorescence[1]

Cell Line: HCT116 cells
Concentration: 5, 10 and 20 μM
Incubation Time: 24 h
Result: Markedly elevated intracellular cholesterol levels.
体内研究
(In Vivo)

Sino-C (30 和 50 mg/kg,腹腔注射,从第 14 天至第 28 天隔日给药一次) 在 HCT116 细胞诱导的 BALB/c 裸鼠模型中表现出显著的抗结直肠癌作用[1]

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

Animal Model: HCT116 cells (1 × 106, s.c.) induce- BALB/c nude mice[1]
Dosage: 30 and 50 mg/kg
Administration: i.t., every other day from day 14 to day 22 (30 mg/kg) then i.t., every other day from day 24 to day 28 (50 mg/kg)
Result: Significantly reduced tumor size and average tumor weight by approximately 43.24%.
Suppressed tumor growth over the two-week study period.
Caused no significant changes in mouse body weight, indicating minimal systemic toxicity.
分子量

506.44

Formula

C25H25Cl2NO4S

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
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  • 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.

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产品名称:
Sino-C
目录号:
HY-179526
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