2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis DNA/RNA Synthesis Bcl-2 Family IAP
  4. ZLMT-72

ZLMT-72 是一种口服有效的双重 CDK2 和 CDK9 抑制剂，其 IC50 值分别为 0.741 nM 和 1.03 nM。ZLMT-72 在激酶谱分析和胆碱酯酶抑制活性方面均表现出良好的选择性。ZLMT-72 对结直肠癌 (CRC) 细胞系 HCT116 具有显著的抗增殖作用 (GI50 < 0.1 nM)。ZLMT-72 通过抑制视网膜母细胞瘤蛋白和 RNA 聚合酶 II (RNA polymerase II) 的磷酸化诱导细胞凋亡 (apoptosis)，从而下调抗凋亡蛋白 (Mcl-1 和 XIAP) 的表达。ZLMT-72 可用于结直肠癌 (CRC) 的研究。

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ZLMT-72

ZLMT-72 Chemical Structure

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ZLMT-72 相关抗体

Top Publications Citing Use of Products

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

查看 Bcl-2 Family 亚型特异性产品:

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

查看 IAP 亚型特异性产品:

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cIAP cIAP-1 cIAP-2 XIAP

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC)[1].

IC50 & Target[1]

CDK2/CycA2

0.741 (IC50)

CDK9/CycT1

1.03 (IC50)

Mcl-1

 

XIAP

 

体外研究
(In Vitro)

ZLMT-72 (1-10 nM；10 天) 完全抑制 HCT116 细胞的克隆形成 [1] 。
ZLMT-72 (1-10 nM；72 小时) 在 HCT116 细胞中表现出强效的抗增殖作用 [1] 。
ZLMT-72 (1-10 nM；48 小时) 在 HCT116 细胞中诱导显著的细胞凋亡[1]。
ZLMT-72 (1-10 nM；24 小时) 显著抑制 HCT116 细胞迁移[1]。
ZLMT-72 (1-10 nM；48 小时) 抑制 CDK2/9 并减少 HCT116 细胞中抗凋亡蛋白的表达[1]。

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

ZLMT-72 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCT116 cells
Concentration: 1 nM, 3.3 nM, 10 nM
Incubation Time: 72 hours
Result: Exhibited potent antiproliferative effects, with GI50 values < 0.1 nM. The compound significantly inhibited cell proliferation.

Cell Proliferation Assay[1]

Cell Line: HCT116 cells
Concentration: 1 nM, 3.3 nM, 10 nM
Incubation Time: 10 days
Result: Completely suppressed colony formation in HCT116 cells at 10 nM, demonstrating strong antiproliferative activity. 

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 10 nM, 3.3 nM, 1 nM
Incubation Time: 48 hours
Result: Induced apoptosis in 30.19% of HCT116 cells at 10 nM, with 23.3% early-stage and 6.89% late-stage apoptosis. 

Cell Migration Assay [1]

Cell Line: HCT116 cells
Concentration: 1 nM, 3.3 nM, 10 nM
Incubation Time: 24 hours
Result: Significantly inhibited HCT116 cell migration at 10 nM and 3.3 nM, with a reduced migration rate.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 10 nM, 3.3 nM, 1 nM
Incubation Time: 48 hours
Result: Significantly downregulated the levels of phosphorylated Rb (p-Rb) and inhibited the phosphorylation of RNA polymerase II at the Ser2 site, indicating CDK2/9 inhibition.
Also reduced the expression of antiapoptotic proteins (MCL-1 and XIAP).
体内研究
(In Vivo)

ZLMT-72 (1.1-10 mg/kg，口服，每日两次，连续 14 天) 在 HCT116 异种移植模型中表现出强大的抗肿瘤疗效，并在皮下和原位肿瘤模型中显示出良好的安全性[1]。

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

Animal Model: Balb/c nude mice bearing HCT116 cells (subcutaneous and orthotopic xenograft tumor models)[1]
Dosage: 10 mg/kg, 3.3 mg/kg, 1.1 mg/kg
Administration: Oral, oral, twice daily, for 14 days
Result: Tumor growth was significantly inhibited in both subcutaneous and orthotopic models.
At 10 mg/kg, tumor growth inhibition (TGI) was 50.6% in subcutaneous models and 84.3% in orthotopic models.
Revealed a significantred reduction in Ki67-positive and CDK20-positive cells.
Tumor weight and volume were significantly reduced, and no significant toxicity was observed.
分子量

485.60

Formula

C29H32FN5O
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

ZLMT-72 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:

ZLMT-72ZLMT72ZLMT 72CDKApoptosisDNA/RNA SynthesisBcl-2 FamilyIAPCyclin dependent kinasecolorectal cancertherapeutic potentialantitumor efficacyCRCHCT116dual CDK2/9 inhibitorCDK2CDK9Inhibitorinhibitorinhibit

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