A PROTAC that drives Cdk9 degradation
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THAL-SNS-032

Item No. 40958

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]amino]carbonyl]-N-[2-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]-1-piperidineacetamide
CAS Number
2139287-33-3
Molecular Formula
C40H52N8O10S2
Formula Weight
869.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/mlMethanol: Slightly Soluble: 0.1-1 mg/ml
SMILES
O=C(C1=C2C=CC=C1NCCOCCOCCOCCNC(CN3CCC(CC3)C(NC4=NC=C(SCC5=NC=C(C(C)(C)C)O5)S4)=O)=O)N(C(C(N6)=O)CCC6=O)C2=O
InChi Code
InChI=1S/C40H52N8O10S2/c1-40(2,3)29-21-43-32(58-29)24-59-33-22-44-39(60-33)46-35(51)25-9-13-47(14-10-25)23-31(50)42-12-16-56-18-20-57-19-17-55-15-11-41-27-6-4-5-26-34(27)38(54)48(37(26)53)28-7-8-30(49)45-36(28)52/h4-6,21-22,25,28,41H,7-20,23-24H2,1-3H3,(H,42,50)(H,44,46,51)(H,45,49,52)
InChi Key
BXDZOYLPNAIDOC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    THAL-SNS-032 is a proteolysis-targeting chimera (PROTAC) containing the cyclin-dependent kinase 2 (Cdk2), Cdk7, and Cdk9 inhibitor SNS-032 (Item No. 17904) linked to a cereblon (CRBN) binding moiety.1 It selectively induces degradation of Cdk9 over Cdk1, Cdk2, and Cdk7 in MOLT-4 cells when used at a concentration of 250 nM. THAL-SNS-032 inhibits human cytomegalovirus (HCMV) replication in infected human foreskin fibroblasts (HFFs; EC50s = 0.025 µM).2 It also inhibits viral replication in murine CMV-infected mouse embryonic fibroblasts (MEFs; EC50 = 0.22 µM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Olson, C.M., Jiang, B., Erb, M.A., et al. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat. Chem. Biol. 14(2), 163-170 (2018).

    2. Hahn, F., Hamilton, S.T., Wangen, C., et al. Development of a PROTAC-based targeting strategy provides a mechanistically unique mode of anti-cytomegalovirus activity. Int. J. Mol. Sci. 22(23), 12858 (2021).