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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 "
PWWP1
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "PWWP1" in MCE Product Catalog:
1
1 Cited Publications
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MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain) [1].
NSD2-IN-1 (compound 38) is a potent and high selective NSD2-PWWP1 (nuclear receptor-binding SET domain 2-PWWP1) inhibitor, with an IC50 of 0.11 μM. NSD2-IN-1 can bind to NSD2-PWWP1 and then affect the expression of genes regulated by NSD2. NSD2-IN-1 induces apoptosis and cell cycle arrest [1].
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UNC6934 is a selective NSD2-PWWP1 antagonist with a Kd of 91 nM against human targets. UNC6934 binds to the canonical methyl-lysine binding pocket of NSD2-PWWP1 and directly competes with H3K36me2 for binding. UNC6934 induces the aggregation of NSD2 within the nucleolus, without altering ribosomal RNA transcription, global H3K36me2 levels or the proliferation of KMS-11 cells. UNC6934 can be used in studies related to multiple myeloma and diffuse intrinsic pontine glioma [1] .
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BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells [1].
Cat. No.: HY-114208
CAS No.: 2387510-86-1
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BI-9321, a chemical probe, is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells [1].
Cat. No.: HY-171119
CAS No.: 2797183-30-1
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NSD2-PWWP1-IN-1 (compound 31) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 0.64 µM. NSD2-PWWP1-IN-1 has the potential for the research of cancer [1].
Cat. No.: HY-171120
CAS No.: 2797183-32-3
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NSD2-PWWP1-IN-2 (compound 33) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 1.49 µM. NSD2-PWWP1-IN-2 has the potential for the research of cancer [1].
Cat. No.: HY-175871
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(Rac)-NSD2-PWWP1-IN-4 (compound 7) is an effective NSD2-PWWP1 inhibitor IC50 and Kd values are 0.21 and 0.15 μM. (Rac)-NSD2-PWWP1-IN-4 can be used in tumor research [1].
Cat. No.: HY-171121
CAS No.: 2797183-35-6
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NSD2-PWWP1-IN-3 (compound 36) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 8.05 µM. NSD2-PWWP1-IN-3 has the potential for the research of cancer [1].
Cat. No.: HY-142048
CAS No.: 2538293-52-4
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BI-9466 (Compound 2) is a nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd of 144 µM. BI-9466 is a negative control compound of BI-9321 (HY-114208). BI-9466 has no inhibitory activity against NSD3-PWWP1 domain by introduction of a much basic nitrogen heterocycle at the 5-position of BI-9321 [1].
Cat. No.: HY-178321
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UNC10088 is a molecular glue targeting NSD2. UNC10088 mediates the formation of a stable ternary complex between SCFFBXO22 and the NSD2 PWWP1 domain. UNC10088 promotes ubiquitination of the SCFFBXO22-dependent NSD2 PWWP1 domain through reversible covalent bonding with the C326 region of FBXO22. UNC10088 could be used in cancer research [1].
Cat. No.: HY-161670
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NSD2-PWWP1 ligand 1 (compound 34) is a small molecule ligand targeting the NSD2-PWWP1 domain (pIC50: 8.2). NSD2 is a large multidomain protein with histone writer and histone reader functions. Dysregulation of the levels of histone methyltransferase nuclear receptor binding SET domain 2 (NSD2) may lead to a variety of hematological and solid malignancies. NSD2-PWWP1 ligand 1 binds to NSD2, reducing its enzymatic activity and inhibiting tumorigenesis [1].
Cat. No.: HY-155817
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UNC7096 (compound 53) is a biotinylated affinity reagent. The phenyl ring of UNC7096 replaces the pyrimidine ring in UNC6934 (HY-145103) and introduces biotin at the para position of the phenyl ring, which has a high binding affinity to the NSD2-PWWP1 domain (Kd=46 nM). UNC7096 blocks the interaction between NSD2-PWWP1 and nucleosomal H3K36me2 by occupying the methyl-lysine binding pocket of NSD2-PWWP1. This binding is achieved by covalent binding through the formation of hydrogen bonds and a specific aromatic cage structure. UNC7096 can be used to capture proteins that interact with the NSD2-PWWP1 domain to further analyze the biological significance of these interactions [1].
Cat. No.: HY-179651
CAS No.: 106664-01-1
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NSD2-PWWP1-IN-6 (Compound 16) is an effective NSD2-PWWP1 inhibitor with a Kd value of 30 nM. NSD2-PWWP1-IN-6 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-6 can be used for cancer research [1].
Cat. No.: HY-179650
CAS No.: 217798-45-3
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NSD2-PWWP1-IN-5 (Compound 13) is an effective NSD2-PWWP1 inhibitor with a Kd value of 78 nM. NSD2-PWWP1-IN-5 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-5 inhibits the proliferation of U2OS osteosarcoma cells and induces cell cycle arrest and apoptosis. NSD2-PWWP1-IN-5 can be used for the study of osteosarcoma [1].
Cat. No.: HY-184968
CAS No.: 3108071-48-0
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PROTAC NSD2 degrader-1 is a PROTAC degrader that selectively targets NSD2, with a DC50 of 0.37 μM. PROTAC NSD2 degrader-1 induces selective degradation of long and short isoforms of NSD2 containing the PWWP1 domain by forming a ternary complex with FBXO22. NSD2 degradation mediated by PROTAC NSD2 degrader-1 depends on the ubiquitin-proteasome system and the neddylation pathway. PROTAC NSD2 degrader-1 can be used in cancer-related research such as non-small cell lung cancer, multiple myeloma and prostate cancer [1].
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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
