1. PROTAC Apoptosis
  2. PROTACs RIP kinase
  3. PROTAC RIPK1 Degrader-1

PROTAC RIPK1 Degrader-1 是一种选择性的 RIPK1 PROTAC 降解剂。PROTAC RIPK1 Degrader-1 降解多种癌细胞系 (如:A375,B16F10 细胞) 中的 RIPK1。PROTAC RIPK1 Degrader-1 增强放疗在同基因和人源化小鼠模型中的抗癌效果。PROTAC RIPK1 Degrader-1 可用于黑色素瘤等癌症的研究。(粉色: RIPK1-ligand-2:HY-175371,蓝色: (S,R,S)-AHPC-Me:HY-112078,粉色 + 黑色: RIPK1 ligand-Linker Conjugate-1: HY-175374,黑色: Bispiperidin-piperazin-acetater: HY-175373)。

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PROTAC RIPK1 Degrader-1

PROTAC RIPK1 Degrader-1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma. (Pink: RIPK1-ligand-2: HY-175371, Blue: (S,R,S)-AHPC-Me: HY-112078, Pink + Black: RIPK1 ligand-Linker Conjugate-1: HY-175374, Black: Bispiperidin-piperazin-acetater: HY-175373)[1].

IC50 & Target[1]

VHL

 

RIPK1

 

体外研究
(In Vitro)

PROTAC RIPK1 Degrader-1 (Compound 225-5) (0-1 μM, 1-20 小时) 通过结合 RIPK1、VHL、蛋白酶体和 Cullin-RING E3 连接酶复合物来诱导 HEK-293T-RIPK1-HiBiT (DC50 < 0.1 nM, Dmax = 93 %)、A375 (DC50 = 41 nM, Dmax = 97 %)、B16F10 (DC50 = 91 nM, Dmax = 92 %)、PC3、LNCap、MCF7、NOMO1、RS$;11、U87 细胞中的 RIPK1 降解[1]

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

Western Blot Analysis[1]

Cell Line: A375, B16F10, PC3, LNCap, MCF7, NOMO1, RS$;11, U87 cells
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 1 h, 2 h, 4 h, 8 h, 16 h, 20 h
Result: Induced RIPK1 degradation.
体内研究
(In Vivo)

PROTAC RIPK1 Degrader-1 (Compound 225-5) (10-50 mg/kg,腹腔注射/静脉注射,每日两次/一次,3-11 天) 可降低 B16F10 C57BL/6 小鼠模型中的 RIPK1 水平[1]
PROTAC RIPK1 Degrader-1 (10-20 mg/kg,腹腔注射,每日一次,3-11 天) 可降低人源化 A375 黑色素瘤 NSG小鼠模型中的 RIPK1 水平[1]

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

Animal Model: B16F10 (0.3 M) C57BL/6 mouse model[1]
Dosage: 50 mg/kg/10 mg/kg
Administration: i.p., twice daily, 3 days/i.v., twice daily, 3 days
Result: Lowered RIPK1 levels.
Animal Model: Humanized (PBMC, 1 × 107) A375 (5 M) melanoma NSG mouse model[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: i.p., once daily, 3 days
Result: Lowered RIPK1 levels.
Animal Model: B16F10 (0.3 M) syngeneic C57BL/6 mouse model[1]
Dosage: 40 mg/kg+20 mg/kg
Administration: i.p., once daily, 3 days+ once daily, 8 days
Result: Delayed tumor growth and extended median survival from 19 to 24 days when used in combination with radiation therapy.
Animal Model: A375 (1 M) humanized (PBMC, 1 × 107) NSG mouse model[1]
Dosage: 20 mg/kg
Administration: i.p., once daily, 11 days
Result: Reduced tumor volume by 89% in combination with radiation therapy.
分子量

1256.63

Formula

C69H85N13O6S2

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 RIPK1 Degrader-1 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.

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产品名称:
PROTAC RIPK1 Degrader-1
目录号:
HY-175370
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