A degrader of NSD2
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UNC8153 (trifluoroacetate salt)

Item No. 38932

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[4-[[[4-[[(6-aminohexyl)amino]carbonyl]phenyl]amino]carbonyl]phenyl]methyl]-N-cyclopropyl-3,4-dihydro-3-oxo-2H-1,4-benzoxazine-7-carboxamide, trifluoroacetate salt
CAS Number
2929304-61-8
Molecular Formula
C33H37N5O5 • CF3COOH
Formula Weight
697.7
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 5 mg/ml
λmax
282 nm
SMILES
O=C1COC2=C(C=CC(C(N(C3CC3)CC4=CC=C(C(NC5=CC=C(C(NCCCCCCN)=O)C=C5)=O)C=C4)=O)=C2)N1.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C33H37N5O5.C2HF3O2/c34-17-3-1-2-4-18-35-31(40)23-9-12-26(13-10-23)36-32(41)24-7-5-22(6-8-24)20-38(27-14-15-27)33(42)25-11-16-28-29(19-25)43-21-30(39)37-28;3-2(4,5)1(6)7/h5-13,16,19,27H,1-4,14-15,17-18,20-21,34H2,(H,35,40)(H,36,41)(H,37,39);(H,6,7)
InChi Key
PRNFABQCXAELBV-UHFFFAOYSA-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

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    Product Description

    UNC8153 is a degrader of the histone-lysine N-methyltransferase NSD2.1 It induces its degradation of NSD2 with a 50% degradation constant (DC50) value of 350 nM and is selective for NSD2 over NSD1 and NSD3 at 20 µM. UNC8153 (10 µM) induces NSD2 degradation and reduces histone H3 lysine 36 dimethylation (H3K36me2) in MM.1S multiple myeloma cells, an effect that can be inhibited by the inhibitor of the ubiquitin-activating enzyme MLN4924 (Item No. 15217). It reduces the proliferation of MM.1S cells expressing NSD2 containing an activating glutamate-to-lysine mutation at position 1099 (NSD2E1099K), but not MDA-MB-231, U2OS, or HEK293 cells expressing wild-type NSD2, when used at a concentration of 20 µM. UNC8153 (20 µM) decreases attachment of MM.1S cells in a migration assay.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hanley, R.P., Nie, D.Y., Tabor, J.R., et al. Discovery of a potent and selective targeted NSD2 degrader for the reduction of H3K36me2. J. Am. Chem. Soc. 145(14), 8176-8188 (2023).