2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Androgen Receptor Apoptosis
  4. SC428

SC428 是雄性激素受体 (AR) 的抑制剂，靶向 AR N-端结构域。SC428 有效地降低了 AR- V7、 ARv567es 以及全长 AR (AR- FL) 及其 LBD 突变体的转激活。SC428 显著抑制雄激素刺激的 AR -FL核易位、染色质结合和 AR 调节的基因转录。SC428 在体外抑制肿瘤细胞的增殖。SC428 在移植 22Rv1 的小鼠体内通过诱导凋亡抑制肿瘤细胞生长。

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SC428 Chemical Structure

SC428 Chemical Structure

CAS No. : 1898232-70-6

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SC428 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1[1].

体外研究
(In Vitro)

SC428 (10 nmol/L- 1μmol/L, 48 h) 在 293T 细胞 (PSA-Luc 实验) 中抑制 AR-V7 (IC50为 0.42 μM) 和 ARv567es (IC50为 1.31 μM) 反式激活活性。
SC428 (5μM, 1 h) 在 LNCaP 细胞 (CETSA 实验) 中逆转 DHT 诱导的 AR-FL 热稳定 (EC50为 0.31 μM)，SC428 以浓度依赖的方式抑制配体诱导的 AR 的激活，是 F887 L 突变体的拮抗剂[1]。
SC428 (1, 2.5 and 5 μmol/L, 30 min) 抑制 LNCaP (IC50为 1.39 μM)，VCaP (IC50为 1.01 μM)， 22Rv1 (IC50为 1.13 μM) AR 阳性细胞系的增殖。AR 阴性细胞株 PC3 (IC50为 6.49 μM) 中抗增殖能力较弱 [1]。
SC428 (5 μmol/L, 5 h) 可减弱LNCaP-AR 细胞 (ChIP 实验) AR 调控基因的转录，阻断AR-FL染色质结合 (共聚焦成像实验)，减少核易位[1]。
SC428 (2.5, 5 μmol/L, 24 h) 抑制高表达 AR- V7 前列腺癌细胞的 AR 信号传导[1]。
SC428 (0.5, 1, 2.5 and 5 μmol/L, 24 h) 对 LNCaP-ARV7 和 LNCaP-ARwt 细胞都有抑制效果 (Enzalutamide (HY-70002) - resistant)，蛋白和 mRNA 水平上抑制 PSA 和 UBE2C (蛋白免疫印迹和 qPCR)[1]。
SC428 (5 mmol/L, 5h) 在 22Rv1 细胞中破坏 AR-V7 二聚体 (免疫沉淀实验) 和核定位 (共聚焦成像技术)[1]。

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

SC428 相关抗体:

Real Time qPCR[1]

Cell Line: LNCaP-AR
Concentration: 5 μmol/L
Incubation Time: 24 h
Result: Inhibited AR-FL transcription significantly and rogen-mediated mRNA expression.

Real Time qPCR[1]

Cell Line: 22Rv1
Concentration: 2.5 and 5 μmol/L
Incubation Time: 24 h
Result: 2.5 mmol/L SC428 reduced AR-regulated gene mRNA to 50% of controls, whereas 5 mmol/L SC428 further reduced it to 10% to 30% of controls. AR-V7-dependent Ar signaling was blocked in 22Rv1 cells.

Real Time qPCR[1]

Cell Line: LNCaP-AR-V7
Concentration: 0.5, 1, 2.5 and 5 μmol/L
Incubation Time: 24 h
Result: Inhibited the expression of PSA gene in LNCaP-AR-V7 cells and significantly decreased the mRNA level of AR-V7 specific gene UBE2C.

Western Blot Analysis[1]

Cell Line: LNCaP-AR-V7
Concentration: 0.5, 1, 2.5 and 5 μmol/L
Incubation Time: 24 h
Result: Inhibited PSA-Luc with equal potency in LNCaP-AR-V7 and LNCaP-ARWT cells.

Western Blot Analysis[1]

Cell Line: LNCaP-AR-V7，22Rv1
Concentration: 5 μmol/L
Incubation Time: 5 h
Result: Reduced AR-V7 homodimer.

Cell Proliferation Assay[1]

Cell Line: LNCaP, VCaP, 22Rv1, PC3
Concentration: 1, 2.5 and 5 μmol/L
Incubation Time: 30 min
Result: Inhibited the proliferation of three AR-positive cell lines, and the anti-proliferation effect of SC428 on the AR-negative cell line PC3 was 6-fold lower than that on the AR-positive cell line.

Cell Proliferation Assay[1]

Cell Line: LNCaP-AR
Concentration: 0.1 μM - 10 μM
Incubation Time: 30 h
Result: Overcame the ENZ-resistant AR signaling and cell proliferation driven by AR-V7.
体内研究
(In Vivo)

SC428 (60 mg/kg; 腹腔注射; 每天一次; 18天) 在通过体内诱导 AR-V7 肿瘤细胞凋亡抑制肿瘤生长[1]。
SC428 (90 mg/kg; 腹腔注射; 每周五次; 3周) 在小鼠体内抑制高表达 AR-V7 的前列腺癌异种移植物的生长[1]。

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

Animal Model: 22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice[1].
Dosage: 60 mg/kg
Administration: Intraperitoneal injection (i.p.) ; daily route 5 days a week; 3 weeks
Result: Reduced the tumor growth by 50% , the mice did not lose weight, and the tumor PSA was reduced to undetectable levels.
Animal Model: 22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice. Male Nu/Nu mice were surgically castrated when the implanted 22Rv1 cells achieved an average tumor size of 200 mm3[1].
Dosage: 90 mg/kg
Administration: Intraperitoneal injection (i.p.); daily route 5 days a week; 3 weeks
Result: Inhibited the growth of prostate cancer with high expression of AR-V7.Good drug tolerance, no significant weight loss.
分子量

337.32

Formula

C15H10F3N3OS
CAS 号
性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

SC428 相关分类

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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.

Keywords:

SC4281898232-70-6SC 428SC-428Androgen ReceptorApoptosisAndrogen receptor inhibitorAR ligand-binding domain (LBD) Prostate cancerResistance mechanismsInhibitorinhibitorinhibit

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