MS453

Catalog No.: A26565
Histone Methyltransferase
MS453 is a potent and selective inhibitor of the histone methyltransferase SETD8, exhibiting an IC50 of 804 nM. It preferentially targets a cysteine residue adjacent to the binding site, demonstrating specificity over 28 other methyltransferases. The crystal structure elucidates the binding mode of MS453 to SETD8, offering valuable insights for the design of advanced chemical probes aimed at this important target in epigenetic regulation.
Grouped product items
Size Price Stock Qty
25mg
$1,275.00
In stock
50mg
$1,625.00
In stock
100mg
$2,000.00
In stock
Bulk Size
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Free Delivery on orders over $500
Research use only. We do not sell to patients.

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Adooq Products cited in reputable paper
Science VOLUME 380, ISSUE 6663 (2023)
Science VOLUME 369, ISSUE 6510 (2020)
Science VOLUME 356, ISSUE 6336 (2017)
Cell Vol. 185 Issue 23 p4428-4447.e28
Cell Vol 177, Issue 7, p1933-1947.e25
Cell Vol 156, Issue 5, p857-1114
Nature Volume 622 Issue 7982 (2023)
Nature volume 620, pages890-897 (2023)
Nature volume 610, pages540-546 (2022)
Nature volume 588, pages83-88 (2020)
Nature volume 574, pages268-272 (2019)
Nature volume 573, pages539-545 (2019)
Nature volume 567, pages118-122 (2019)
Nature volume 551, pages639-643 (2017)
Nature volume 551, pages247-250 (2017)
Nature volume 548, pages356-360 (2017)
Nature volume 545, pages187-192 (2017)
Biological Activity
DescriptionMS453 is a potent and selective inhibitor of the histone methyltransferase SETD8, exhibiting an IC50 of 804 nM. It preferentially targets a cysteine residue adjacent to the binding site, demonstrating specificity over 28 other methyltransferases. The crystal structure elucidates the binding mode of MS453 to SETD8, offering valuable insights for the design of advanced chemical probes aimed at this important target in epigenetic regulation.
Product Information
Catalog NumA26565
FormulaC20H27N5O3
Molecular Weight385.46
CAS Number2059892-29-2
SMILESCOC1=C(C=C(C2=C1)N=C(N=C2NCCCNC(C=C)=O)N3CCCC3)OC
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