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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
17 Results for "
nuclear receptor-binding SET domain
" in MedChemExpress (MCE) Product Catalog:
Products (17)
17 Results for "nuclear receptor-binding SET domain" in MCE Product Catalog:
2
2 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) .
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1 Cited Publications
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MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease .
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 .
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UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
Cat. No.: HY-161574
CAS No.: 3061315-33-8
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LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)) .
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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 .
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UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
Cat. No.: HY-162308
CAS No.: 744260-15-9
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NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis .
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 .
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 .
PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.
Cat. No.: HY-170674
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ND-L11B is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with the DC50 of 1.48 and 0.8 μM, the Dmax is closed to 80 % .
Cat. No.: HY-170674A
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ND-L11B TFA is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with the DC50 of 1.48 and 0.8 μM, the Dmax is closed to 80 % .
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 .
Cat. No.: HY-177400
CAS No.: 3034213-62-9
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NSD-IN-5 is a nuclear receptor-binding SET domain (NSD) inhibitor with IC50 values of 6 nM and < 1 nM against NSD1 and NSD2, respectively. NSD-IN-5 can be used in research related to multiple myeloma .
Cat. No.: HY-P702074
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: NSD2; nuclear receptor binding SET domain Protein 2; WHSC1; MMSET; KMT3G; Histone-Lysine N-Methyltransferase NSD2; nuclear SET domain-Containing Protein 2; Wolf-Hirschhorn Syndrome Candidate 1; TRX5; Multiple Myeloma SET domain Containing Protein Type III
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P87049
Synonyms: FLJ23286 antibody; IL5 promoter REII region binding protein antibody; KIAA1090 antibody; MGC176638 antibody; MMSET antibody; MMSET type II antibody; Multiple myeloma SET domain containing protein type III antibody; Multiple myeloma SET domain protein antibody; Multiple myeloma SET domain-containing protein antibody; NSD 2 antibody; FLJ23286 antibody; IL5 promoter REII region binding protein antibody; KIAA1090 antibody; MGC176638 antibody; MMSET antibody; MMSET type II antibody; Multiple myeloma SET domain containing protein type III antibody; Multiple myeloma SET domain protein antibody; Multiple myeloma SET domain-containing protein antibody; NSD 2 antibody; NSD2 antibody; NSD2_HUMAN antibody; nuclear receptor binding SET domain protein 2 antibody; nuclear SET domain-containing protein 2 antibody; Probable histone-lysine N-methyltransferase NSD2 antibody; Protein trithorax-5 antibody; REIIBP antibody; Trithorax/ash1 related protein 5 antibody; TRX5 antibody; TRX5 protein antibody; WHS antibody; Whsc1 antibody; Wolf Hirschhorn syndrome candidate 1 antibody; Wolf Hirschhorn syndrome candidate 1 protein antibody; Wolf-Hirschhorn syndrome candidate 1 protein antibody;
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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
