2. PROTAC Apoptosis Cell Cycle/DNA Damage
  3. Ligands for E3 Ligase CDK Apoptosis Molecular Glues
  4. 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.

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NCT02 Chemical Structure

NCT02 Chemical Structure

CAS No. : 790245-61-3

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Based on 1 publication(s) in Google Scholar

NCT02 Related Antibodies

Top Publications Citing Use of Products

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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Description

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].

IC50 & Target

Cereblon-DDB1

 

In Vitro

NCT02 (0-20 μM; 72 h) inhibits cell viability in colorectal cancer cell lines (TSC03, TSC08, TSC47, etc.) in a dose-dependent manner and has low toxicity to normal fibroblasts[1].
NCT02 (10 μM; 24-48 h) induces apoptosis in TSC03 and TSC14 cells, as evidenced by a significant increase in the proportion of lysed PARP-positive cells[1].
NCT02 (10 μM; 6 h) triggers the degradation of CCNK/CDK12 complex and significantly reduces CCNK protein levels, accompanied by a decrease in p-Ser2 POLR2 phosphorylation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NCT02 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human colorectal cancer spheroids (TSC03, TSC08, TSC47, etc.), normal primary fibroblasts (HD-F)
Concentration: 0, 0.1, 1, 10, 20 μM
Incubation Time: 72 h
Result: Significantly reduced viability of cancer cells in a dose-dependent manner, with IC50s ranging from 2.5-5.8 μM in sensitive TSCs (e.g., TSC03, TSC08).
Molecular Weight

312.39

Formula

C17H16N2O2S
CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (160.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2011 mL 16.0056 mL 32.0113 mL
5 mM 0.6402 mL 3.2011 mL 6.4023 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2011 mL 16.0056 mL 32.0113 mL 80.0282 mL
5 mM 0.6402 mL 3.2011 mL 6.4023 mL 16.0056 mL
10 mM 0.3201 mL 1.6006 mL 3.2011 mL 8.0028 mL
15 mM 0.2134 mL 1.0670 mL 2.1341 mL 5.3352 mL
20 mM 0.1601 mL 0.8003 mL 1.6006 mL 4.0014 mL
25 mM 0.1280 mL 0.6402 mL 1.2805 mL 3.2011 mL
30 mM 0.1067 mL 0.5335 mL 1.0670 mL 2.6676 mL
40 mM 0.0800 mL 0.4001 mL 0.8003 mL 2.0007 mL
50 mM 0.0640 mL 0.3201 mL 0.6402 mL 1.6006 mL
60 mM 0.0534 mL 0.2668 mL 0.5335 mL 1.3338 mL
80 mM 0.0400 mL 0.2001 mL 0.4001 mL 1.0004 mL
100 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8003 mL
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NCT02 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NCT02790245-61-3NCT 02NCT-02Ligands for E3 LigaseCDKApoptosisMolecular GluesE3 ligase-recruiting MoietyCyclin dependent kinasecyclin Kproteasomal degradationCCNKubiquitinationCDK12metastatic colorectal cancerInhibitorinhibitorinhibit

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