2. Cell Cycle/DNA Damage Apoptosis GPCR/G Protein MAPK/ERK Pathway
  3. G-quadruplex Bcl-2 Family c-Myc Ras
  4. NSC 373981

NSC 373981 是 CARD11 G4 稳定剂。NSC 373981 在细胞中能够稳定 CARD11 G4 结构并抑制 CARD11 的转录。NSC 373981 也抑制 BCL2 和 MYC。NSC 373981 可抑制 KRAS 和 TERT 的转录。NSC 373981 对弥漫大 B 细胞淋巴瘤具有抗癌活性。

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NSC 373981

NSC 373981 Chemical Structure

CAS No. : 95455-02-0

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NSC 373981 相关抗体

Top Publications Citing Use of Products

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NSC 373981 is a CARD11 G4 stabilizer. NSC 373981 stabilizes the CARD11 G4 structure and inhibits CARD11 transcription in cells. NSC 373981 also inhibits BCL2 and MYC. NSC 373981 suppresses the transcription of KRAS and TERT. NSC 373981 exhibits anticancer activity against diffuse large B-cell lymphoma[1][2].

IC50 & Target[1]

BCL2

 

K-RAS

 

体外研究
(In Vitro)

NSC 373981 (24 h; 37°C) 在酸性、中性和碱性条件下均表现出稳定性，且在 37°C 下孵育 24 小时后，在小鼠血浆中也保持稳定[1]。
NSC 373981 (2.5-10.0 µM; 24 h) 以剂量依赖方式抑制 RIVA、HBL1 和 HT 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞中 CARD11、BCL2 和 MYC 的 mRNA 表达；在 RIVA 和 HT 细胞中还对 KRAS 和 TERT 产生作用，但对 VAL DLBCL 细胞或 GM22671 良性 B 细胞中的 CARD11 表达无影响[2]。
NSC 373981 (0.02-40 µM; 72 h) 在 RIVA、HT 和 GM22671 细胞中表现出低微摩尔级别的细胞毒性，在其能抑制多种癌基因 mRNA 水平的细胞中细胞毒性更高，且该细胞毒性与基础 CARD11 表达无相关性[2]。

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

NSC 373981 相关抗体:

Real Time qPCR[2]

Cell Line: ABC DLBCL (RIVA, HBL1), GCB DLBCL (HT, VAL), benign GC B (GM22671) cells
Concentration: 2.5, 5.0, 10.0 µM
Incubation Time: 24 h
Result: Caused a significant, dose-dependent repression of CARD11 mRNA levels (45-90% reduction at 10 µM) in RIVA, HBL1, and HT cells.
Induced concurrent dose-dependent decreases in BCL2 and MYC mRNA levels in RIVA, HBL1, and HT cells.
Reduced KRAS mRNA by 25-30% in RIVA cells and TERT mRNA by 40-55% in HT cells at 10 µM.
Showed no significant change in CARD11 mRNA levels in VAL and GM22671 cells.
Reduced MYC mRNA in GM22671 cells at 10 µM.
体内研究
(In Vivo)

NSC 373981 (37.5-150 mg/kg；静脉注射、腹腔注射；单次) 在雄性无胸腺 nu/nu 小鼠中表现出独特的动力学特征，腹腔注射生物利用度为 58%，且在多种体液中可检测到 I 相和 II 相代谢物[1]。

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

Animal Model: athymic nu/nu (male)[1]
Dosage: 37.5 mg/kg (i.v.); 150 mg/kg (i.p.)
Administration: i.v.; single dose; i.p.; single dose
Result: Achieved peak plasma concentration >5.9 μg/mL, terminal elimination half-life 1.2 hours, volume of distribution 694 mL, and plasma clearance 390 mL/hr following i.v. administration.
Reached peak plasma concentration 2.1 μg/mL at 15 minutes, terminal elimination half-life 36.8 hours, and 58% bioavailability following i.p. administration.
Detected multiple Phase I and Phase II metabolites in plasma, urine, feces, and bile, including those from aromatic nitro group reduction, primary alcohol moiety oxidation, benzylic hydroxylation, naphthalene moiety hydroxylation/dihydrodiol formation, and Phase II conjugation reactions.
分子量

257.24

Formula

C14H11NO4
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

NSC 373981 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:

NSC 37398195455-02-0NSC373981NSC-373981G-quadruplexBcl-2 Familyc-MycRasMycTERTdiffuse large B cell lymphomaHT DLBCL cellsHBL1 cellsKRASBCL2CARD11MYCRIVA cellsbenign germinal center B cellsInhibitorinhibitorinhibit

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