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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
139 Results for "
SET domain
" in MedChemExpress (MCE) Product Catalog:
Products (139)
139 Results for "SET domain" in MCE Product Catalog:
14
14 Publications Verification
Cat. No.: HY-18627A
CAS No.: 1627607-87-7
Synonyms: (R)-PFI-2 hydrochloride
Target:
Research Areas:
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC50 value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis .
14
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Research Areas:
PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride, a chemical probe, is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC50 value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis .
6
6 Cited Publications
Cat. No.: HY-141539A
Purity: 99.77%
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Research Areas:
SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD .
6
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NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
2
2 Cited Publications
Cat. No.: HY-N5024
CAS No.: 173932-75-7
Category:
Ketones, Aldehydes, Acids Guttiferae Extract Phenols Polyphenols Plants Garcinia hanburyi Hook. f. Disease Research Fields Cancer
Target:
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) .
2
2 Cited Publications
Cat. No.: HY-P74394
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: VTCN1; V-SET domain Containing T Cell Activation Inhibitor 1; B7-H4; B7H4; B7h.5; B7S1; B7x; V-SET domain-Containing T-Cell Activation Inhibitor 1; Immune Costimulatory Protein B7-H4; B7 Superfamily Member 1; B7 Family Member, H4; B7 Homolog 4; FLJ22418; T Cell Costimulatory Molecule B7x; T-Cell Costimulatory Molecule B7x; Protein B7S1; PRO1291; VCTN1
Species:
Mouse
Source:
HEK293
1
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 .
1
1
1 Cited Publications
Cat. No.: HY-P76079
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: SMYD2; Histone Methyltransferase SMYD2; SET And MYND domain Containing 2; ZMYND14; HSKM-B; Lysine N-Methyltransferase 3C; KMT3C; [Histone H3]-Lysine(4) N-Trimethyltransferase; SET And MYND domain-Containing Protein 2; Zinc Finger, MYND domain Containing 1
Species:
Human
Source:
Sf9 insect cells
1
1 Cited Publications
Cat. No.: HY-P72428
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: VSIR; V-SET Immunoregulatory Receptor; C10orf54; SISP1; VISTA; B7-H5; PD-1H; Dies1; GI24; B7H5; V-Type Immunoglobulin domain-Containing Suppressor Of T-Cell Activation; V-SET domain-Containing Immunoregulatory Receptor; V-domain Ig Suppressor Of T Cell Ac
Species:
Mouse
Source:
HEK293
1
1 Cited Publications
Cat. No.: HY-P74613
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: KMT5A; Lysine N-Methyltransferase 5A; Prev. SETD8; H4-K20-HMTase KMT5A; PR-SET7; PR/SET07; SET07; [Histone H4]-Lysine(20) N-Methyltransferase; SET8; H4-K20-Specific Histone Methyltransferase; SET domain Containing (Lysine Methyltransferase) 8; Histone-Lys
Species:
Human
Source:
E. coli
1
1 Cited Publications
Cat. No.: HY-P74395
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: VTCN1; V-SET domain Containing T Cell Activation Inhibitor 1; B7-H4; B7H4; B7h.5; B7S1; B7x; V-SET domain-Containing T-Cell Activation Inhibitor 1; Immune Costimulatory Protein B7-H4; B7 Superfamily Member 1; B7 Family Member, H4; B7 Homolog 4; FLJ22418;
Species:
Human
Source:
HEK293
1
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Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM .Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents .Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma .
Research Areas:
Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM. Ryuvidine also inhibits KDM5A and blocks DNA synthesis. Ryuvidine has anticancer activity against tumors such as breast cancer. Ryuvidine improves arthritis .
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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 .
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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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AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78 μM .
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 .
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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 .
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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
