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TMX-2138

TMX-2138 is a CDKs PROTAC degrader, with IC50s of 8.7 nM, 10.9 nM, 7.0 nM and 25.7 nM for CDK1/cyclinB, CDK2/cyclinA, CDK5/p25 and CDK9/cyclinT1, respectively. TMX-2138 promotes ubiquitination and degradation of CDKs. TMX-2138 can be used for the research of ovarian cancer (Pink: CDKs ligand (HY-151071) ; Blue: E3 ligase CRBN ligand (HY-14658) ; Black: linker (HY-W008352) ) [1].

Product Specifications

CAS Number

[2488892-07-3]

UNSPSC

12352005

Target

CDK; PROTACs

Related Pathways

Cell Cycle/DNA Damage; PROTAC

Field of Research

Cancer

Smiles

O=C(C1=C(NC2=NC(NC3=CC=C(S(=O)(NCCOCCOCCOCCOCCNC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=O)C=C3)=NC=C2Br)C=CC=C1F)N

Molecular Formula

C40H43BrFN9O11S

Molecular Weight

956.79

References & Citations

[1]Teng M, et al. Development of CDK2 and CDK5 Dual Degrader TMX-2172. Angew Chem Int Ed Engl. 2020 Aug 10;59 (33) :13865-13870.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

CDK1; CDK2; CDK4; CDK5; CDK6; CDK7; CDK9

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