MAP4K1/HPK1 Degrader
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PROTAC HPK1 Degrader-3
0 ImagesCat. No.: HY-162816Purity: 98.11%PROTAC HPK1 Degrader-3 is an orally active, PROTAC degrader that selectively targets HPK1, with a DC50 of 21.26 nM. PROTAC HPK1 Degrader-3 induces HPK1 degradation via the ubiquitin-proteasome system and forms a stable ternary complex with HPK1 and CRBN. It inhibits the SLP76 and NF-κB signaling pathways, enhances MAPK signal transduction, reverses the immunosuppressive factor-mediated inhibition of T cell cytokine secretion, and promotes the secretion of T cell immune cytokines. PROTAC HPK1 Degrader-3 suppresses tumor growth and enhances anti-PD-L1-mediated antitumor activity. It can be used in studies related to malignant tumors, such as colorectal cancer.
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PROTAC HPK1 Degrader-1
0 ImagesPROTAC HPK1 Degrader-1 (compound B1) is a PROTAC degrader that recruits cereblon to induce HPK1 degradation, with a DC50 of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits HPK1 kinase activity, with an IC50 of 140.5 nM. PROTAC HPK1 Degrader-1 suppresses the phosphorylation of SLP76 protein, with an IC50 of 496.1 nM. PROTAC HPK1 Degrader-1 can be used to investigate non-kinase-dependent signaling of HPK1 in the TCR pathway and cancer-related research.
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SS47
0 ImagesCat. No.: HY-146231CAS No.: 2636072-62-1SS47 is a hematopoietic progenitor kinase HPK1 PROTAC-class degrader and immune activator. SS47 promotes the proliferation of CD4+ and CD8+ T cells as well as IFN-γ secretion, and enhances the anti-tumor cytotoxicity and in vivo efficacy of BCMA CAR-T cells. SS47 also inhibits tumor growth in mouse models, and when combined with anti-PD-1 therapy, it improves the immune response of 4T1 tumor-bearing mice. SS47 can be used in breast cancer-related research.
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DD205-291
0 ImagesCat. No.: HY-168282CAS No.: 3047066-15-6DD205-291 is a selective, orally active HPK1 PROTAC degrader with a DC50 of 8.8 nM. By inducing complete degradation of HPK1 protein, DD205-291 simultaneously blocks both its kinase-dependent functions and non-kinase scaffold functions. DD205-291 inhibits the phosphorylation of SLP-76 with an EC50 of 22.98 nM. DD205-291 induces the production of IL-2 and IFN-γ with EC50 values of 34.68 nM and 32.6 nM, respectively. Combined with anti-PD1 in mouse models, DD205-291 exerts tumor-suppressive effects with favorable safety profiles. DD205-291 can be used in colon cancer-related research.
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PROTAC HPK1 Degrader-8
0 ImagesCat. No.: HY-184230CAS No.: 3120899-50-2PROTAC HPK1 Degrader-8 is a HPK1 PROTAC degrader with a DC50 of 1-10 nM. PROTAC HPK1 Degrader-8 promotes HPK1 ubiquitination and degradation. PROTAC HPK1 Degrader-8 induces IL-2 production, with an EC50 of 3 nM. PROTAC HPK1 Degrader-8 can be used in research related to hematologic malignancies and solid tumors.
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PROTAC HPK1 Degrader-4
0 ImagesCat. No.: HY-174135PROTAC HPK1 Degrader-4 is an orally active HPK1 PROTAC degrader and immune activator, with DC50 values of 3.16 nM and 72.59 nM in Jurkat cells and PBMCs, respectively. PROTAC HPK1 Degrader-4 induces degradation via the ubiquitin-proteasome system, downregulates the HPK1-SLP76 signaling pathway, reduces the phosphorylation level of SLP76 (S376), and promotes immune activation. PROTAC HPK1 Degrader-4 can be used in the research of colorectal cancer and B-cell lymphoma.
