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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 "
SETDB1
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "SETDB1" in MCE Product Catalog:
6
6 Cited Publications
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Research Areas:
SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (Kd of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer [1] .
6
6 Cited Publications
Cat. No.: HY-141539A
Purity: 99.77%
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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 [1] .
Cat. No.: HY-173156
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UNC10013 is an inhibitor targeting the triple Tudor domain (3TD) of SETDB1. UNC10013 covalently binds to Cys385 of SETDB1 3TD, acts as a negative allosteric modulator of the methyltransferase domain of SETDB1, reduces the level of Akt methylation mediated by SETDB1, and blocks Tyr308 phosphorylation of Akt. UNC10013 is applicable to cancer-related research [1].
Cat. No.: HY-168992
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UNC6535 is a covalent ligand targeting the SETDB1 triple Tudor domain (3TD) with negative allosteric modulator properties, with an IC50 of 3.4 μM and a Kd of 4.2 μM. UNC6535 inhibits the methyltransferase activity of recombinant SETDB1 protein lacking the 3TD domain. UNC6535 reversibly binds to the aromatic cages of both TD2 and TD3 subdomains of SETDB1 3TD simultaneously, displacing the endogenous H3K9Me2K14Ac histone tail ligand. UNC6535 can be used in research on cancer and neurodegenerative diseases [1] .
Cat. No.: HY-RS12748
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SETDB1 Human Pre-designed siRNA Set A contains three designed siRNAs for SETDB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-RS23131
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Setdb1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Setdb1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-RS16697
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Setdb1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Setdb1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-184362
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P-SETDB1-4 is a SETDB1 PROTAC degrader with a Kd of 86 nM. P-SETDB1-4 recruits CRBN to SETDB1, induces proteasome-dependent degradation of SETDB1, and forms a ternary complex with CRBN to achieve targeted degradation. P-SETDB1-4 reduces DNA synthesis. P-SETDB1-4 exhibits anticancer activity against breast cancer. P-SETDB1-4 can be used in breast cancer-related research [1].
Cat. No.: HY-185849
CAS No.: 2585194-96-1
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SETDB1-IN-1 is a SETDB1 inhibitor with an IC50 of 16 μM. SETDB1-IN-1 inhibits histone methyltransferase) activity via SAM-competitive and peptide-dependent mechanisms. SETDB1-IN-1 is applicable to research related to melanoma, lung cancer, liver cancer, breast cancer and prostate cancer [1].
Cat. No.: HY-168992A
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Research Areas:
UNC6535 TFA is a covalent ligand targeting the triple Tudor domain (3TD) of SETDB1. UNC6535 TFA reversibly binds to the aromatic cages of both TD2 and TD3 within SETDB1 3TD simultaneously, weakly inhibits the methyltransferase activity of SETDB1, and displaces the H3K9Me2K14Ac peptide from SETDB1 3TD [1].
Cat. No.: HY-P703071
Purity: ≥ 80%, as determined by reducing SDS-PAGE.
Synonyms: KMT1E; Histone-lysine N-methyltransferase SETDB1; ERG-associated protein with SET domain (ESET); Histone H3-K9 methyltransferase 4 (H3-K9-HMTase 4); Lysine N-methyltransferase 1E; SET domain bifurcated 1; SETDB1; ESET
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Cat. No.: HY-P85154
Synonyms: SETDB1; KIAA0067; KMT1E; Histone-lysine N-methyltransferase SETDB1; ERG-associated protein with SET domain; ESET; Histone H3-K9 methyltransferase 4; H3-K9-HMTase 4; Lysine N-methyltransferase 1E; SET domain bifurcated 1
Cat. No.: HY-P703604
Purity: ≥ 80%, as determined by reducing SDS-PAGE.
Synonyms: ESET; KIAA0067; KMT1E
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Source:
Cat. No.: HY-181914
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UNC7242 is an antagonist that binds to the Tudor domains of PHF1 and PHF19, with a Kd of 1.13 μM for PHF1 and 0.64 μM for PHF19. UNC7242 fails to displace full-length PHF1 or PHF19 from H3K36me3 nucleosomes or chromatin. UNC7242 can be used in studies related to multiple myeloma, endometrial stromal sarcoma, and ossifying fibromyxoid tumor [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
