Histone Methyltransferase Antagonist
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BI-9321 trihydrochloride
0 ImagesBI-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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UNC6934
0 ImagesUNC6934 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.
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UNC1215
0 ImagesUNC1215, a chemical probe, is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a Kd value of 120 nM and an IC50 of 40 nM. UNC1215 has the potential to treat malignant brain tumor.
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NV03
0 ImagesNV03 is a potent and selective antagonist of Ubiquitin-like with PHD and RING finger domains 1 (UHRF1)-H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 is also a ligand for E3 ligase. NV03 can be studied in anticancer research.
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UNC4976 TFA
0 ImagesCat. No.: HY-126327APurity: 98.3%UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
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UNC4976
0 ImagesCat. No.: HY-126327CAS No.: 2920299-34-7UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
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BI-9321
0 ImagesCat. No.: HY-114208CAS No.: 2387510-86-1BI-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.
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SARS-CoV-2 nsp14-IN-1
0 ImagesCat. No.: HY-150680CAS No.: 2816165-02-1SARS-CoV-2 nsp14-IN-1 (Compound 3) is a prototypic bisubstrate inhibitor of SARS-CoV-2 Nsp14 MTase with an IC50 value of 0.061 μM. SARS-CoV-2 nsp14-IN-1 (Compound 3) has an excellent selectivity profile over a panel of human methyltransferases, can against apanel of 10 human MTases including histone lysine, proteinarginine, and DNA and RNA MTases.
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UNC7242
0 ImagesCat. No.: HY-181914UNC7242 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.
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BI-9466
0 ImagesCat. No.: HY-142048CAS No.: 2538293-52-4BI-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.
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