A degrader of AR mRNA
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Enantiomer(s)
42092(S)-SKBG-1
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(R)-SKBG-1

Item No. 42091

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R)-4-(2-chloroacetyl)-N-[(4-methoxyphenyl)methyl]-1-[(4-methoxyphenyl)sulfonyl]-2-piperazinecarboxamide
CAS Number
2955634-67-8
Molecular Formula
C22H26ClN3O6S
Formula Weight
496.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
COC(C=C1)=CC=C1CNC([C@H]2CN(C(CCl)=O)CCN2S(C3=CC=C(OC)C=C3)(=O)=O)=O
InChi Code
InChI=1S/C22H26ClN3O6S/c1-31-17-5-3-16(4-6-17)14-24-22(28)20-15-25(21(27)13-23)11-12-26(20)33(29,30)19-9-7-18(32-2)8-10-19/h3-10,20H,11-15H2,1-2H3,(H,24,28)/t20-/m1/s1
InChi Key
SXQZEMXQTRNLRZ-HXUWFJFHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 µg

    $219

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    Cayman Chemical
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    Product Description

    (R)-SKBG-1 is a degrader of mRNA encoding the androgen receptor (AR).1 It decreases mRNA levels of AR and AR splice variant seven (AR-V7) and protein levels of AR and AR-V7 in 22Rv1 prostate cancer cells when used at a concentration of 20 µM. (R)-SKBG-1 (20 µM) reduces protein levels of AR and AR-V7 in wild-type 22Rv1 cells but not in NONO-/- 22Rv1 cells, which lack the RNA-binding protein non-POU domain-containing octamer-binding protein (NONO). It increases the number of NONO nuclear foci and NONO-bound immature mRNA transcripts in 22Rv1 cells. (R)-SKBG-1 is cytotoxic to 22Rv1 cells (IC50 = 44 µM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kathman, S.G., Koo, S.J., Lindsey, G.L., et al. Remodeling oncogenic transcriptomes by small molecules targeting NONO. Nat. Chem. Biol. 19(7), 825-836 (2023).