2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt NF-κB Apoptosis
  3. JAK STAT NF-κB Bcl-2 Family
  4. TM-233

TM-233 是 JAK/STAT 和 NF-κB 信号通路的抑制剂，具有显著的抗肿瘤活性。TM-233 通过抑制 JAK2 和 STAT3 的磷酸化，来降低抗凋亡蛋白 Mcl-1 的表达，并通过直接结合 Mcl-1 基因启动子来调控其转录。此外，TM-233 通过抑制 NF-κB 的 DNA 结合活性，来阻止其从细胞质向细胞核的转位，从而减少 NF-κB 的核内表达。TM-233 在克服 Bortezomib (HY-10227) 耐药性方面展现出潜力，可应用于多发性骨髓瘤领域研究。

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TM-233 Chemical Structure

TM-233 Chemical Structure

CAS No. : 1103745-28-3

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规格 是否有货
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TM-233 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

查看 STAT 亚型特异性产品:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TM-233 is an inhibitor of the JAK/STAT and NF-κB signaling pathways, exhibiting significant antitumor activity. TM-233 reduces the expression of the anti-apoptotic protein Mcl-1 by inhibiting the phosphorylation of JAK2 and STAT3, and regulates its transcription by directly binding to the Mcl-1 gene promoter. Additionally, TM-233 prevents the translocation of NF-κB from the cytoplasm to the nucleus by inhibiting its DNA-binding activity, thereby reducing nuclear NF-κB expression. TM-233 shows potential in overcoming Bortezomib (HY-10227) resistance and can be applied in research related to multiple myeloma[1].

IC50 & Target

JAK2

 

Stat-3

 

Mcl-1

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HL-60 IC50
0.12 μM
Compound: 18
Cytotoxicity against human HL60 cells assessed as growth inhibition after 3 days
Cytotoxicity against human HL60 cells assessed as growth inhibition after 3 days
[PMID: 25801158]
IM-9 IC50
0.23 μM
Compound: 18
Cytotoxicity against human IM9 cells assessed as growth inhibition after 3 days
Cytotoxicity against human IM9 cells assessed as growth inhibition after 3 days
[PMID: 25801158]
分子量

384.42

Formula

C25H20O4
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

TM-233 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

TM-2331103745-28-3TM233TM 233JAKSTATNF-κBBcl-2 FamilyJanus kinaseNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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目录号：
HY-119009
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