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THAL SNS 032 - ≥98%(HPLC), high purity , CAS No.2139287-33-3, Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of cyclin dependent kinase 7;Inhibitor of cyclin dependent kinase 9

  • Moligand™
  • ≥98%(HPLC)
Item Number
T287611
Grouped product items
SKUSizeAvailabilityPrice Qty
T287611-5mg
5mg
In stock
$380.90
T287611-10mg
10mg
In stock
$685.90
T287611-25mg
25mg
In stock
$1,543.90
T287611-50mg
50mg
In stock
$2,777.90

Potent and selective Cdk9 degrading PROTAC

Basic Description

SynonymsN-(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
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPROTAC®comprising the cyclin-dependent kinase inhibitorSNS 032 conjugated to the cereblon E3 ligase ligand,thalidomide. Potent, selective and cereblon-dependent degrader of Cdk9 (EC50= 4 nM). Displays >15-fold selectivity for Cdk9 over other CDKs (EC50val
Storage TempStore at -20°C,Argon charged
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of cyclin dependent kinase 7;Inhibitor of cyclin dependent kinase 9
Product Description

Product description

THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN)


Associated Targets

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK7 Tchem Cyclin-dependent kinase 7 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK16 Tchem Cyclin-dependent kinase 16 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK11B Tchem Cyclin-dependent kinase 11B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK4 Tclin Cyclin-dependent kinase 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CCNT1 Tchem Cyclin-T1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK19 Tchem Cyclin-dependent kinase 19 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CRBN Tclin Protein cereblon 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK6 Tclin Cyclin-dependent kinase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

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
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)
InChi Key BXDZOYLPNAIDOC-UHFFFAOYSA-N
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
Isomeric 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
PubChem CID 131801483
Molecular Weight 869.02

Certificates

Certificate of Analysis(COA)

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8 results found

Lot NumberCertificate TypeDateItem
G23201170Certificate of AnalysisJun 25, 2023 T287611
G23201171Certificate of AnalysisJun 25, 2023 T287611
G23201174Certificate of AnalysisJun 25, 2023 T287611
G23201175Certificate of AnalysisJun 25, 2023 T287611
G23201178Certificate of AnalysisJun 25, 2023 T287611
G23201179Certificate of AnalysisJun 25, 2023 T287611
G23201182Certificate of AnalysisJun 25, 2023 T287611
G23201183Certificate of AnalysisJun 25, 2023 T287611

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 86.9, Max Conc. mM: 100

Related Documents

References

1. Olson CM, Jiang B, Erb MA, Liang Y, Doctor ZM, Zhang Z, Zhang T, Kwiatkowski N, Boukhali M, Green JL et al..  (2018)  Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation..  Nat Chem Biol,  14  (2): (163-170).  [PMID:29251720]

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