THAL SNS 032 - CAS 2139287-33-3

THAL SNS 032 is a potent and selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand conjugated to a cereblon E3 ligase ligand thalidomide. THAL SNS 032 was showed to inhibit proliferation of leukemia cell lines.

* Please be kindly noted that our services and products can only be used for research to organizations or companies and not intended for any clinical or individuals.

Molecular Formula
C40H52N8O10S2
Molecular Weight
869.04

THAL SNS 032

    • Specification
      • Purity
        ≥98%
        Shelf Life
        2 years
        Storage
        Store at -20°C
        IUPAC Name
        N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]-1-[2-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethylamino]-2-oxoethyl]piperidine-4-carboxamide
        Synonyms
        N-(5-(((5-(tert-butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxo-6,9,12-trioxa-3-azatetradecyl)piperidine-4-carboxamide; 1-Piperidineacetamide, 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]-; SNS-THAL-032; Thal-SNS-032; THAL-SNS-032
    • Properties
      • Density
        1.40±0.1 g/cm3
        InChI Key
        BXDZOYLPNAIDOC-UHFFFAOYSA-N
        InChI
        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)
        Canonical SMILES
        CC(C)(C)C1=CN=C(O1)CSC2=CN=C(S2)NC(=O)C3CCN(CC3)CC(=O)NCCOCCOCCOCCNC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O
    • Reference Reading
      • 1. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.
        Olson, C.M., Jiang, B., Erb, M.A., Liang, Y., Doctor, Z.M., Zhang, Z., Zhang, T., Kwiatkowski, N., Boukhali, M., Green, J.L. and Haas, W., 2018. Nature chemical biology, 14(2), pp.163-170.
        Cyclin-dependent kinase 9 (CDK9), an important regulator of transcriptional elongation, is a promising target for cancer therapy, particularly for cancers driven by transcriptional dysregulation. We characterized NVP-2, a selective ATP-competitive CDK9 inhibitor, and THAL-SNS-032, a selective CDK9 degrader consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN). To our surprise, THAL-SNS-032 induced rapid degradation of CDK9 without affecting the levels of other SNS-032 targets. Moreover, the transcriptional changes elicited by THAL-SNS-032 were more like those caused by NVP-2 than those induced by SNS-032. Notably, compound washout did not significantly reduce levels of THAL-SNS-032-induced apoptosis, suggesting that CDK9 degradation had prolonged cytotoxic effects compared with CDK9 inhibition. Thus, our findings suggest that thalidomide conjugation represents a promising strategy for converting multi-targeted inhibitors into selective degraders and reveal that kinase degradation can induce distinct pharmacological effects compared with inhibition.
Bio Calculators
Stock concentration: *
Desired final volume: *
Desired concentration: *

L

* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
g/mol
g
Related Products
BOC Sciences Support

Please contact us with any specific requirements and we will get back to you as soon as possible.


  • Verification code

We invite you to contact us at or through our contact form above for more information about our services and products.

USA
  • International:
  • US & Canada (Toll free):
  • Email:
  • Fax:
UK
  • Email:
Inquiry Basket