2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs CDK Apoptosis
  4. HEMTAC CDK4/6 degrader 1

HEMTAC CDK4/6 degrader 1 是由 HSP90 的配体和 CDK4/6 连接的 PROTAC，Kd 值为 35.7 μM。HEMTAC CDK4/6 degrader 1 在 B16F10 黑色素瘤细胞中诱导 CDK4/6 降解。HEMTAC CDK4/6 degrader 1 将细胞周期阻滞在 G0/G1 期并诱导细胞凋亡。HEMTAC CDK4/6 degrader 1 可用于癌症研究。

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HEMTAC CDK4/6 degrader 1 Chemical Structure

HEMTAC CDK4/6 degrader 1 Chemical Structure

CAS No. : 2821803-61-4

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HEMTAC CDK4/6 degrader 1 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1]. HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

CDK4

 

CDK6

 

体外研究
(In Vitro)

HEMTAC CDK4/6 degrader 1 (compound 26; 0.01-1 μM; 24 h) induces CDK4 and CDK6 degradation in the treated B16F10 cells with a DC50 value (the drug concentration that results in 50% protein degradation) of approximately 26 and 19 nM and a Dmax (maximal percent degradation) of 88 and 92%, respectively[1].
HEMTAC CDK4/6 degrader 1 (0.01-100 μM; 72 h) has anti-proliferative activity against a broad range of human cancer cell lines[1].
HEMTAC CDK4/6 degrader 1 (250 nM; 24 or 48 h) induces B16F10 cells to undergo apoptosis in a dose-dependent manner and arrests cell cycle at G0/G1 phase[1].

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

HEMTAC CDK4/6 degrader 1 相关抗体:

Cell Viability Assay[1]

Cell Line: B16F10, A375, HepG2, MDA-MB-231, and A549 cells
Concentration: 0.01-100 μM
Incubation Time: 72 hours
Result: Inhibited cell growth in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: B16F10 cells
Concentration: 250 nM
Incubation Time: 48 hours
Result: Induced cell apoptosis in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: B16F10 cells
Concentration: 250 nM
Incubation Time: 48 hours
Result: Increased the amount of B16F10 cells in the G0/G1 phase.

Western Blot Analysis[1]

Cell Line: B16F10 cells
Concentration: 0.01, 0.05, 0.1, 0.5, and 1 μM
Incubation Time: 24 hours
Result: Induced CDK4/6 degradation in a dose-dependent manner.
体内研究
(In Vivo)

HEMTAC CDK4/6 degrader 1 (compound 26; 20 and 40 mg/kg; i.p.; daily, for 15 d) has antitumor efficacy in C57BL/6J mice bearing B16F10 melanoma xenografts[1].

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

Animal Model: C57BL/6J mice bearing B16F10 melanoma xenografts[1]
Dosage: 20 and 40 mg/kg
Administration: intraperitoneal injection; daily, for 15 days
Result: Inhibited tumor growth and resulted in fewer CDK4/6-positive cells and led to much more necrosis.
分子量

953.49

Formula

C48H53ClN16O4
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

HEMTAC CDK4/6 degrader 1 相关分类

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  • 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:

HEMTAC CDK4/6 degrader 12821803-61-4PROTACsCDKApoptosisCyclin dependent kinaseB16F10 melanoma cellsanticancercell cycleG0/G1 phaseInhibitorinhibitorinhibit

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