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PROTAC HPK1 Degrader-5
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Catalog No. T212062
PROTACHPK1 Degrader-5 is a potent, orally active HPK1 PROTAC degrader with a DC50 of 5.0 nM and a Dmax of at least 99%. It significantly inhibits HPK1 by degrading it, reducing SLP76 phosphorylation, and enhancing ERK pathway activation, which in turn stimulates the release of IL-2 and IFN-γ. This compound effectively counteracts immune suppression induced by PGE2, NECA, or TGF-β. Alone, PROTACHPK1 Degrader-5 is capable of suppressing tumor growth in MC38 syngeneic mouse models. It is used in research for immunotherapy applications in cancers such as colorectal cancer.
PROTAC HPK1 Degrader-5
PROTAC HPK1 Degrader-5
😃Good
Catalog No. T212062
PROTACHPK1 Degrader-5 is a potent, orally active HPK1 PROTAC degrader with a DC50 of 5.0 nM and a Dmax of at least 99%. It significantly inhibits HPK1 by degrading it, reducing SLP76 phosphorylation, and enhancing ERK pathway activation, which in turn stimulates the release of IL-2 and IFN-γ. This compound effectively counteracts immune suppression induced by PGE2, NECA, or TGF-β. Alone, PROTACHPK1 Degrader-5 is capable of suppressing tumor growth in MC38 syngeneic mouse models. It is used in research for immunotherapy applications in cancers such as colorectal cancer.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
| Description | PROTACHPK1 Degrader-5 is a potent, orally active HPK1 PROTAC degrader with a DC50 of 5.0 nM and a Dmax of at least 99%. It significantly inhibits HPK1 by degrading it, reducing SLP76 phosphorylation, and enhancing ERK pathway activation, which in turn stimulates the release of IL-2 and IFN-γ. This compound effectively counteracts immune suppression induced by PGE2, NECA, or TGF-β. Alone, PROTACHPK1 Degrader-5 is capable of suppressing tumor growth in MC38 syngeneic mouse models. It is used in research for immunotherapy applications in cancers such as colorectal cancer. |
| In vitro | PROTAC HPK1 Degrader-5 (Compound 10m) at 30 nM, after 24 hours, facilitates the degradation of HPK1 in Jurkat cells, relying on the ubiquitin-proteasome system (UPS), CRBN, HPK1, and CRBN. At a concentration of 10 nM, this compound significantly and dose-dependently inhibits phosphorylation of SLP76 in Jurkat cells and in PBMCs stimulated with anti-CD3/CD28 antibodies, while enhancing activation of extracellular signal-regulated kinase (ERK), which aligns with HPK1 degradation. |
| In vivo | PROTAC HPK1 Degrader-5 (Compound 10m), administered orally at doses of 0.5-3 mg/kg every other day for 14 days, significantly inhibits tumor growth in MC38 syngeneic mouse models. When combined with a PD-1 inhibitor, it achieves superior antitumor effects. |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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