2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. PROTAC SMARCA2/4 degrader-38

PROTAC SMARCA2/4 degrader-38 是一种 SMARCA2/4 PROTAC 降解剂 (DC50 分别为: 3.0 nM 和 4.0 nM)。PROTAC SMARCA2/4 degrader-38 能促进 SMARCA2/4 的泛素化和降解。PROTAC SMARCA2/4 degrader-38 可阻断 G0/G1 细胞周期和诱导细胞凋亡 (apoptosis)。PROTAC SMARCA2/4 degrader-38 可用于急性髓系白血病 (AML) 的研究。(粉色：SMARCA2/4 配体；蓝色：VHL 配体 (HY-112078)；黑色：连接子；靶蛋白配体-连接体结合物 (HY-173343))。

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PROTAC SMARCA2/4 degrader-38 Chemical Structure

PROTAC SMARCA2/4 degrader-38 Chemical Structure

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PROTAC SMARCA2/4 degrader-38 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC50: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343))[1].

IC50 & Target[1]

SMARCA2

3.0 nM (DC50)

SMARCA4

4.0 nM (DC50)

VHL

 

体外研究
(In Vitro)

PROTAC SMARCA2/4 degrader-38 (Compound A11) (25-100 nM, 3 天) 可抑制 AML 细胞中 MV-4-11 细胞株 (IC50: 4.9 nM) 和 MOLM-13 细胞株 (IC50: 23.3 nM)，和弥漫大 B 细胞淋巴瘤中 SU-DHL-4 (IC50: 87.7 nM) 和 WSU-DLCL-2 (IC50: 336.7 nM) 的增殖活性[1]。
PROTAC SMARCA2/4 degrader-38 (100-1000 nM, 48 小时) 以浓度依赖性方式诱导 MV-4-11 和 MOLM-13 细胞周期停滞于 G0/G1 期[1]。
PROTAC SMARCA2/4 degrader-38 (100-1000 nM, 72 小时) 可诱导 MV-4-11 和 MOLM-13 细胞凋亡[1]。
PROTAC SMARCA2/4 degrader-38 (11.1-1000 nM, 24 小时) 以浓度依赖性方式抑制 AML 癌基因的转录表达[1]。

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

PROTAC SMARCA2/4 degrader-38 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MV-4-11 cells and MOLM-13 cells
Concentration: 100 nM, 300 nM and 1000 nM
Incubation Time: 48 h
Result: Induced a large accumulation of G0/G1 cells in MV-4-11 and MOLM-13 cells.

Apoptosis Analysis[1]

Cell Line: MV-4-11 cells and MOLM-13 cells
Concentration: 100 nM, 300 nM and 1000 nM
Incubation Time: 72 h
Result: Induced apoptosis in MV-4-11 and MOLM-13 cells.

Western Blot Analysis[1]

Cell Line: MOLM-13 cells; MV-4-11 cells
Concentration: 100 nM, 300 nM and 1000 nM; 11.1 nM, 33.3 nM, 100 nM, 300 nM and 1000 nM
Incubation Time: 72 h; 24 h
Result: Up-regulated apoptosis-related cleaved poly ADP-ribose polymerase (PARP) and cleaved caspase-3 proteins levels.
Down-regulated MYC protein level.

RT-PCR[1]

Cell Line: MV-4-11 cells
Concentration: 11.1 nM, 33.3 nM, 100 nM, 300 nM and 1000 nM
Incubation Time: 24 h
Result: Down-regulated the expression of E2F1, CDC25A, TRAP1, PU. 1, CD44 and BCL-2 genes.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat 1 mg/kg i.v. Cmax 1953 ng/mL
Rat 10 mg/kg p.o. Cmax 6.41 ng/mL
Rat 1 mg/kg i.v. Tmax 0.033 hr
Rat 10 mg/kg p.o. Tmax 0.42 hr
Rat 1 mg/kg i.v. T1/2 1.91 hr
Rat 10 mg/kg p.o. T1/2 2.10 hr
Rat 1 mg/kg i.v. AUC0-t 358 ng·h/mL
Rat 10 mg/kg p.o. AUC0-t 8.22 ng·h/mL
Rat 1 mg/kg i.v. MRT0-t 0.70 hr
Rat 10 mg/kg p.o. MRT0-t 0.81 hr
Rat 10 mg/kg p.o. F 0.62 %
分子量

773.94

Formula

C43H47N7O5S
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

PROTAC SMARCA2/4 degrader-38 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:

PROTAC SMARCA2/4 degrader-38PROTACsEpigenetic Reader DomainApoptosisAnticancerMV-4-11MOLM-13SU-DHL-4WSU-DLCL-2AMLInhibitorinhibitorinhibit

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产品名称：
PROTAC SMARCA2/4 degrader-38
目录号：
HY-173333
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