2. Stem Cell/Wnt Apoptosis
  3. Smo Hedgehog Gli Apoptosis Caspase
  4. SMO-IN-6

SMO-IN-6 是一种 SMO 抑制剂，其 IC50 为 0.12 μM。SMO-IN-6 通过抑制 Hedgehog/GLI 通路，抑制癌细胞增殖、抑制集落形成、诱导细胞凋亡 (apoptosis)。SMO-IN-6 下调肿瘤组织中的 Ki67 与 SOX2 表达，并上调剪切型半胱天冬酶 3 (cleaved-caspase 3) 的表达。SMO-IN-6 可用于皮肤鳞状细胞癌的研究。

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SMO-IN-6

SMO-IN-6 Chemical Structure

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SMO-IN-6 相关抗体

Top Publications Citing Use of Products

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma[1].

体外研究
(In Vitro)

SMO-IN-6 (Compound 16) (72 h) 可强效抑制 A431 皮肤鳞状细胞癌细胞的增殖，其 GI50 为 1.4 μM，相对于非肿瘤性 HaCaT 皮肤细胞的治疗指数为 31[1]。
SMO-IN-6 (1-4 μM; 14 day) 呈剂量依赖性抑制 A431 皮肤鳞状细胞癌细胞的长期集落形成，在 4 μM 时抑制率超过 95%[1]。
SMO-IN-6 (1 μM) 可强效下调 A431 皮肤鳞状细胞癌细胞中 Hedgehog/GLI 通路靶基因 Gli1、Gli2、Ptch1 和 HHip 的表达[1]。
SMO-IN-6 (1-4 μM; 16 h) 可剂量依赖性诱导 A431 皮肤鳞状细胞癌细胞发生凋亡，在 4 μM 浓度下细胞凋亡率达 93%[1]。

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

SMO-IN-6 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A431 cutaneous squamous cell carcinoma cells
Concentration: 1, 2 and 4 μM
Incubation Time: 14 day
Result: Inhibited A431 colony formation in a dose-dependent manner: 1 μM reduced colony formation by over 50%, and 4 μM inhibited over 95% of colony formation.

Apoptosis Analysis[1]

Cell Line: A431 cutaneous squamous cell carcinoma cells
Concentration: 1, 2 and 4 μM
Incubation Time: 16 h
Result: Induced apoptosis in A431 cells in a dose-dependent manner: 1 μM induced apoptosis in 38% of cells, 2 μM in 54% of cells, and 4 μM in up to 93% of cells.
体内研究
(In Vivo)

SMO-IN-6 (Compound 16) (10-25 mg/kg；腹腔注射；给药 2 天停药 1 天；14 天) 可剂量依赖性地抑制 BALB/c 裸鼠的皮肤鳞状细胞癌肿瘤生长[1]。

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

Animal Model: BALB/c nude mice (female, 6-8 weeks old, 18-20 g, subcutaneously injected with A431 cells)[1]
Dosage: 10 mg/kg; 25 mg/kg
Administration: i.p.; 2on1off dosing regimen; 14 days
Result: Achieved a tumor growth inhibition (TGI) rate of 30%.
Achieved a TGI rate of 56%.
Induced ~40% TUNEL-positive apoptotic cells.
Significantly downregulated GLI1, Ki67, and SOX2 levels in tumor tissues.
Significantly upregulated cleaved-caspase 3 levels in tumor tissues.
Caused no significant body weight loss, morphological abnormalities in major organs, or hematological toxicity.
分子量

449.37

Formula

C23H26Cl2N2O3
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

SMO-IN-6 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:

SMO-IN-6SmoHedgehogGliApoptosisCaspaseSmoothenedGLI2NIH-3T3 Shh Light II cellsSMOHedgehog/GLI signalingGLI1HHipHaCaT nontumoral skin cellsPtch1A431 cutaneous squamous cell carcinoma cellsInhibitorinhibitorinhibit

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