A PROTAC that drives BRD7 and BRD9 degradation
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VZ 185

Item No. 41454

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,4R)-N-(2-((5-(4-(2,6-dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)piperazin-1-yl)pentyl)oxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide
CAS Number
2306193-61-1
Molecular Formula
C53H67FN8O8S
Formula Weight
995.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
CN1C=C(C(C=C2OC)=CC(OC)=C2CN(CC3)CCN3CCCCCOC(C=C(C(SC=N4)=C4C)C=C5)=C5CNC([C@H](C[C@H]6O)N(C6)C([C@H](C(C)(C)C)NC(C7(CC7)F)=O)=O)=O)C8=CC=NC=C8C1=O
InChi Code
InChI=1S/C53H67FN8O8S/c1-33-46(71-32-57-33)34-11-12-35(27-56-48(64)42-26-37(63)29-62(42)50(66)47(52(2,3)4)58-51(67)53(54)14-15-53)43(23-34)70-22-10-8-9-17-60-18-20-61(21-19-60)31-41-44(68-6)24-36(25-45(41)69-7)40-30-59(5)49(65)39-28-55-16-13-38(39)40/h11-13,16,23-25,28,30,32,37,42,47,63H,8-10,14-15,17-22,26-27,29,31H2,1-7H3,(H,56,64)(H,58,67)/t37-,42+,47-/m1/s1
InChi Key
ZAGCLFXBHOXXEN-JPTLTNPLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

    $455

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    Product Description

    VZ 185 is a proteolysis-targeting chimera (PROTAC) composed of a von Hippel-Lindau (VHL) ligand and bromodomain-containing protein 7 (BRD7)- and BRD9-binding ligand.1 It is selective for BRD7 and BRD9 over 6,273 other proteins at 100 nM. VZ 185 degrades BRD7 and BRD9 with half-maximal degradation concentration (DC50) values of 4.5 and 1.8 nM, respectively, in a cell-free assay. It decreases BRD7 and BRD9 levels in HeLa cells by 10 and 14%, respectively, when used at a concentration of 1 µM. VZ 185 reduces the proliferation of EoL-1 leukemia and A-204 sarcoma cells (IC50s = 3.4 and 39 nM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zoppi, V., Hughes, S.J., Maniaci, C., et al. Iterative design and optimization of initially inactive proteolysis targeting chimeras (PROTACs) identify VZ185 as a potent, fast, and selective von hippel-lindau (VHL) based dual degrader probe of BRD9 and BRD7. J. Med. Chem. 62(2), 699-726 (2019).