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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
16 Results for "
SLP76 phosphorylation
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "SLP76 phosphorylation" in MCE Product Catalog:
2
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Research Areas:
ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a +CD8 + T cells, but not T cells, PD-1 +CD8 + T cells, TIM-3 +CD8 + Infiltration of T cells and LAG3 +CD8 + T cells was reduced .
Cat. No.: HY-163372
CAS No.: 3034182-97-0
PROTAC 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 .
Cat. No.: HY-160940
CAS No.: 2810880-82-9
HPK1-IN-46 (Compound 36) is an efficient and highly selective HPK1 reverse indazole inhibitor with an IC50 value of 1.1 nM. HPK1-IN-46 exhibits high selectivity for CDK2, JAK1, and JAK2. HPK1-IN-46 inhibits SLP76 phosphorylation mediated by HPK1, reverses T-cell inhibition, and enhances anti-tumor immunity. HPK1-IN-46 can be used in immunotherapy research for tumors .
Cat. No.: HY-161335
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HPK1-IN-43 (compound 9f) is a HPK1 kinase inhibitor with the IC50 value of 0.32 nM. HPK1-IN-43 inhibits the phosphorylation of the downstream protein SLP-76 and enhances the secretion of interleukin-2 (IL-2) and interferon-γ (IFN-γ). HPK1-IN-43 can be used in cancer research .
Cat. No.: HY-172594
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HPK1-IN-57 (Compound 10c) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 value of 0.09 nM. HPK1-IN-57 inhibits the activity of HPK1 kinase, hindering the phosphorylation of the downstream adaptor protein SLP76 (IC50 is 33.74 nM) and effectively stimulating the secretion of the T cell activation marker IL-2 (EC50 is 84.24 nM). HPK1-IN-57 is promising for research of tumor immunotherapy .
Cat. No.: HY-168282
CAS No.: 3047066-15-6
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DD205-291 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 .
Cat. No.: HY-179111
CAS No.: 3034320-17-4
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HPK1-IN-64 is a potent, selective, and orally active HPK1 inhibitor with an IC50 value of 1.9 nM. HPK1-IN-64 exhibits selectivity exceeding 100-fold, 80-fold, 300-fold, and 350-fold against off-target kinases such as GLK, MAP4K5, TBK1, and TNIK, respectively. HPK1-IN-64 inhibits SLP76 protein phosphorylation and IL-2 secretion. HPK1-IN-64 may be used in cancer research, such as for colorectal cancer .
Cat. No.: HY-175547
CAS No.: 3108744-13-1
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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 .
Cat. No.: HY-184745
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HPK1-IN-71 is a potent and selective HPK1 inhibitor with an IC50 of 26.3 nM. HPK1-IN-71 can inhibit the phosphorylation of SLP76, promote the secretion of IL-2 and show high selectivity for other kinases and immune-targeting kinases. HPK1-IN-71 can be used in colon cancer research .
Cat. No.: HY-179727
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PROTAC HPK1 Degrader-7 (compound D02) is a potent and selective PROTAC HPK1 degrader with an DC50 of 3.07 nM. PROTAC HPK1 Degrader-7 exhibits selectivity over GLK. PROTAC HPK1 Degrader-7 induces HPK1 degradation in a CRBN- and proteasome-dependent manner. PROTAC HPK1 Degrader-7 inhibits SLP-76 phosphorylation, induces IL-2 and IFN-γ secretion in human primary T cells. PROTAC HPK1 Degrader-7 can be used for immunology research .
Cat. No.: HY-182238
CAS No.: 3095423-83-6
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HPK1-IN-69 is an orally active HPK1 inhibitor with an IC50 of 1.7 nM. HPK1-IN-69 inhibits the HPK1-mediated TCR signaling pathway, reduces the phosphorylation level of SLP76, and promotes the release of IL-2. HPK1-IN-69 exhibits in vivo anti-tumor activity in mouse models. HPK1-IN-69 can be used for the research of colorectal cancer and MC38 syngeneic tumors .
Cat. No.: HY-179338
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HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC50 value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC50 of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC50 of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research .
Cat. No.: HY-181924
CAS No.: 3078477-58-1
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HPK1-IN-68 (Compound 39) is a HPK1 inhibitor with an IC50 of 2.8 nM. HPK1-IN-68 blocks HPK1 signaling, inhibits HPK1-mediated phosphorylation of SLP76, and promotes the production of the IL-2 cytokine. HPK1-IN-68 antagonizes the immunosuppressive effect mediated by PGE2. HPK1-IN-68 enhances the infiltration of CD3 +/CD8 + T cells into tumor tissues. HPK1-IN-68 exerts T cell-dependent antitumor efficacy in a mouse colon cancer model. HPK1-IN-68 exhibits significant synergistic antitumor effects when used in combination with anti-PD-1. HPK1-IN-68 is applicable to research related to colon cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
