NCT02

NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models[1][2][3].

Product Specifications

CAS Number

[790245-61-3]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Apoptosis; CDK; Ligands for E3 Ligase; Molecular Glues

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/nct02.html

Purity

98.14

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(NC1=NC=C(C)S1)CC2=COC3=CC4=C(CCC4)C=C32

Molecular Formula

C17H16N2O2S

Molecular Weight

312.39

Precautions

H315, H319, H335

References & Citations

[1]Dieter SM, et al. Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer. Cell Rep. 2021;36 (3) :109394.|[2]Lei P, et al. Current progress and novel strategies that target CDK12 for drug discovery. Eur J Med Chem. 2022 Oct 5;240:114603.|[3]Weagel E G, et al. Molecular glues: enhanced protein-protein interactions and cell proteome editing. Medicinal Chemistry Research, 2022, 31 (7) : 1068-1087.