2. PROTAC MAPK/ERK Pathway Stem Cell/Wnt Immunology/Inflammation
  3. PROTACs MAP4K ERK Interleukin Related IFNAR
  4. PROTAC HPK1 Degrader-5

PROTAC HPK1 Degrader-5 是一种强效且具有口服活性的 HPK1 PROTAC 降解剂 (DC50 = 5.0 nM; Dmax ≥ 99%)。PROTAC HPK1 Degrader-5 通过降解 HPK1 显著抑制 SLP76 磷酸化并增强 ERK 通路活化，从而刺激 IL-2 和 IFN-γ 的释放。PROTAC HPK1 Degrader-5 能够克服 PGE2、NECA 或 TGF-β 引起的免疫抑制作用。PROTAC HPK1 Degrader-5 单独使用即可有效抑制 MC38 同基因小鼠模型中的肿瘤生长。PROTAC HPK1 Degrader-5 可用于肿瘤 (如结直肠癌) 免疫治疗的研究 (粉色：靶蛋白配体 (HY-175549)；蓝色：E3 连接酶配体 (HY-W023573)；黑色：Linker；E3 连接酶配体 + Linker (HY-175551))。

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PROTAC HPK1 Degrader-5

PROTAC HPK1 Degrader-5 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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Customer Review

PROTAC HPK1 Degrader-5 相关抗体

Top Publications Citing Use of Products

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

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ERK ERK1 ERK2 ERK5 ERK8

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy (Pink: Target protein ligand (HY-175549); Blue: E3 ligand (HY-W023573); Black: Linker; E3 ligand + Linker (HY-175551))[1].

IC50 & Target[1]

ERK

 

IL-2

 

Cereblon

 

体外研究
(In Vitro)

PROTAC HPK1 Degrader-5 (Compound 10m) (30 nM, 24 h) 在 Jurkat 细胞诱导 HPK1 降解，需要泛素-蛋白酶体系统 (UPS)、CRBN、HPK1 和 CRBN 的参与[1]。
PROTAC HPK1 Degrader-5 (10 nM) 显著且剂量依赖性地抑制 Jurkat 细胞和抗 CD3/CD28 抗体刺激的 PBMC 中直接下游 SLP76 的磷酸化，并增强远端下游细胞外信号调节激酶 (ERK) 的活化，这与 HPK1 降解一致[1]。

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

PROTAC HPK1 Degrader-5 相关抗体:

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 30 nM
Incubation Time: 24 h
Result: Degraded HPK1 and can be inhibited by MG132 (HY-13259), MLN4924 (HY-70062), and Thalidomide (HY-14658).
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 2 mg/kg i.v. CL 2.40 mL/min/kg
Mice 20 mg/kg p.o. Tmax 11.7 h
Mice 2 mg/kg i.v. Vss 1.42 L/kg
Mice 20 mg/kg p.o. T1/2 18.3 h
Mice 2 mg/kg i.v. T1/2 6.81 h
Mice 20 mg/kg p.o. Cmax 1527 ng/mL
Mice 2 mg/kg i.v. AUClast 12770 ng·h/mL
Mice 20 mg/kg p.o. AUClast 26758 ng·h/mL
Mice 2 mg/kg i.v. AUCinf 14043 ng·h/mL
Mice 20 mg/kg p.o. AUCinf 48715 ng·h/mL
Mice 2 mg/kg i.v. MRT 8.95 h
Mice 20 mg/kg p.o. F 21.0 %
体内研究
(In Vivo)

PROTAC HPK1 Degrader-5 (Compound 10m) (0.5-3 mg/kg，口服，每隔一天一次，持续 14 天) 显著抑制 MC38 同基因肿瘤小鼠模型中的肿瘤生长，并与 PD-1 阻断剂联合使用时可达到更优异的抗肿瘤效果[1]。

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

Animal Model: MC38 xenografts model established insix-week-old female C57BL/6 mice[1]
Dosage: 0.5, 1.5 and 3 mg/kg
Administration: orally administration (p.o.), every other day for 14 days
Result: Achieved a superior antitumor effect when combined with PD-1 blockade mAb
Combined with anti-PD-1 mAb achieved significantly enhanced antitumor efficacy.
Was tolerated with no significant body weight loss and mortality observed during the treatment period.
Alone or combined with anti-PD-1 induced weakened nucleus-to-cytoplasm, remarkable nuclear shrinkage and extensive tumor cell death.
Significantly increased CD8+ T cell infiltration, exceeding anti-PD-1 mAb at 1.5 mpk.
分子量

795.89

Formula

C43H45N11O5
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 HPK1 Degrader-5 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 HPK1 Degrader-5PROTACsMAP4KERKInterleukin RelatedIFNARMAPK Kinase Kinase KinaseExtracellular signal regulated kinasesILInterferon-α/β receptorInterferon-alpha/beta receptorPROTACtumor immunotherapymice modelPD-1Jurkat cellsInhibitorinhibitorinhibit

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