2. Neuronal Signaling Cell Cycle/DNA Damage Others
  3. Choline Kinase Early 2 Factor (E2F) Fluorescent Dye
  4. JAS239

JAS239 是一种可透过血脑屏障的 ChoK 抑制剂。JAS239 可抑制磷酸胆碱合成，降低 E2F1 蛋白表达水平。JAS239 具有近红外荧光特性。JAS239 对胶质母细胞瘤具有抗肿瘤活性。JAS239 可用于胶质母细胞瘤的相关研究。

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JAS239

JAS239 Chemical Structure

CAS No. : 1630288-74-2

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JAS239 相关抗体

Top Publications Citing Use of Products

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CHKα

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JAS239 is a blood-brain barrier-permeable ChoK inhibitor. JAS239 inhibits phosphocholine synthesis and reduces the expression level of E2F1 protein. JAS239 exhibits near-infrared fluorescence properties. JAS239 exerts anti-tumor activity against glioblastoma. JAS239 can be used in studies related to glioblastoma[1][2][3].

IC50 & Target[1]

ChoK

 

E2F1

 

体外研究
(In Vitro)

JAS239 (100 μM max; 24 h) 可降低胶质母细胞瘤 (GBM) 细胞的代谢活性 (细胞活力的替代指标)，在常氧和低氧条件下对 F98、9L、U-87 MG 和 U-251 MG 细胞系的作用效力相近[2]。
JAS239 (500 nM; 24-96 h) 可通过诱导细胞周期阻滞并下调 E2F-1 表达来抑制 GBM 细胞的增殖[2]。
JAS239 (500 nM; 0-96 h) 可在常氧条件下抑制 9L 胶质母细胞瘤细胞系的增殖[3]。

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

JAS239 相关抗体:

Cell Invasion Assay[2]

Cell Line: rat F98, human U-87 MG GBM cell lines (3D spheroid assay); rat F98, 9L, human U-251 MG GBM cell lines (integrin expression analysis)
Concentration: 500 nM
Incubation Time: 16 h (3D spheroid assay)
Result: Significantly reduced track straightness (0.28 ± 0.11 vs.
0.32 ± 0.12, p < 0.0001), track length (84.0 ± 48.0 μm vs.
113.2 ± 86 μm, p < 0.0001), and average speed (0.005 ± 0.001 μm/s vs.
0.007 ± 0.004 μm/s, p < 0.0001), and induced super-diffusive cell motion in normoxic F98 spheroids.
Significantly reduced track straightness and length, and increased cell speed, with induced super-diffusive cell motion in DMOG-hypoxic F98 spheroids.
Significantly increased track length (133.0 ± 61.6 μm vs.
120.7 ± 57.7 μm, p < 0.001) and average speed (0.007 ± 0.001 μm/s vs.
0.006 ± 0.001 μm/s, p < 0.0001), with no change in track straightness, and induced super-diffusive cell motion in normoxic U-87 MG spheroids.
Resulted in track straightness and speed comparable to DMOG-only treatment, with induced super-diffusive cell motion in DMOG-hypoxic U-87 MG spheroids.
Reduced integrin α3β1 protein expression (a marker of cell mobility) in F98, 9L, and U-251 MG cells.
体内研究
(In Vivo)

JAS239 (4 mg/kg；腹腔注射；每日 1 次；连续 5 天) 可抑制胶质母细胞瘤大鼠和小鼠的肿瘤生长[1]。

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

Animal Model: Fischer F344 (female, weight 100-120 g, intracranial injection of 50,000 F98 GBM cells)[1]
Dosage: 4 mg/kg
Administration: intraperitoneal injection; once daily; 5 consecutive days
Result: Significantly reduced tumor growth (p < 0.05) and percentage change of tumor volume (p = 0.033) compared to controls.
Detected a significant reduction (p = 0.02) in mI/tCr ratio in treated tumors.
Noted a 32% non-significant reduction in Glx/tCr ratio.
Observed a near-significant 97% increase (p = 0.052) in (Lip + Lac)/tCr ratio.
Measured a near-significant lower mitotic index (p = 0.06) in treated tumors.
Showed non-significant reduction in tCho/tCr ratio and non-significant trend of reduction in tCho/NAA ratio.
Animal Model: Fischer F344 (female, weight 100-120 g, intracranial injection of 100,000 9L GBM cells)[1]
Dosage: 4 mg/kg
Administration: intraperitoneal injection; once daily; 5 consecutive days
Result: Observed non-significant tumor growth arrest compared to controls.
Measured the largest non-significant reduction in tCho/tCr ratio (-42%) across all models.
Detected a significant reduction (p = 0.047) in tCho/NAA ratio.
Showed non-significant trend of reduction in mI/tCr ratio and Glx/tCr ratio.
Observed a non-significant -20% change in (Lip + Lac)/tCr ratio.
Measured a lower mitotic index in treated tumors.
Animal Model: C57BL/6 (male, age 8-10 weeks, weight 20-25 g, intracranial injection of 500,000 GL261 GBM cells)[1]
Dosage: 4 mg/kg
Administration: intraperitoneal injection; once daily; 5 consecutive days
Result: Observed non-significant tumor growth arrest compared to controls.
Showed non-significant reduction in tCho/tCr ratio and non-significant trend of reduction in tCho/NAA ratio.
Detected non-significant trend of reduction in mI/tCr ratio.
Noted no significant change in Glx/tCr ratio and (Lip + Lac)/tCr ratio.
Measured a lower mitotic index in treated tumors.
分子量

505.10

Formula

C31H37ClN2O2
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

JAS239 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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:

JAS2391630288-74-2JAS 239JAS-239Choline KinaseEarly 2 Factor (E2F)Fluorescent DyeCKChoKcholine phosphokinaseU-87 MGphosphatidylcholine synthesisG0/G1 cell cycle arrestglioblastoma9Lapoptosisblood-brain barriercholine kinase alphaF98U-251 MGInhibitorinhibitorinhibit

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