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Cat. No.: HY-189062

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ZJC-11

ZJC-11 is a CDK7 inhibitor with an IC₅₀ of 5.4 nM. ZJC-11 binds covalently to CDK7, inhibits CDK7-dependent phosphorylation of RNAPII at Ser2, Ser5 and Ser7 sites, and suppresses transcriptional processes. ZJC-11 acts as a cell cycle inhibitor, inhibits the G2/M checkpoint pathway, and induces G2/M phase arrest. ZJC-11 induces DNA damage-driven cellular senescence and cell death. ZJC-11 exhibits antiproliferative activity against triple-negative breast cancer both in vitro and in vivo. ZJC-11 can be used for research related to triple-negative breast cancer

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화학식: C₂₉H₂₈ClN₇O₂
분자량:542.03

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

ZJC-11 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

CDK7

5.4 nM (IC₅₀)

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC50	0.60 μM	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay. Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay.	42593900
CAL-148	IC50	2.41 μM	Antiproliferative activity against human CAL-148 cells assessed as reduction in cell viability by MTT assay. Antiproliferative activity against human CAL-148 cells assessed as reduction in cell viability by MTT assay.	42593900
MDA-MB-231	IC50	627.9 nM	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs assessed as reduction in cell viability by MTT assay. Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs assessed as reduction in cell viability by MTT assay.	42593900
MDA-MB-231	IC50	540.0 nM	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs assessed as reduction in cell viability by MTT assay. Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs assessed as reduction in cell viability by MTT assay.	42593900
MDA-MB-468	IC50	634.7 nM	Antiproliferative activity against human MDA-MB-468 cells incubated for 48 hrs assessed as reduction in cell viability by MTT assay. Antiproliferative activity against human MDA-MB-468 cells incubated for 48 hrs assessed as reduction in cell viability by MTT assay.	42593900
MDA-MB-468	IC50	305.7 nM	Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs assessed as reduction in cell viability by MTT assay. Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs assessed as reduction in cell viability by MTT assay.	42593900
ZR-75-1	IC50	2177 nM	Antiproliferative activity against human ZR-75-1 cells incubated for 48 hrs assessed as reduction in cell viability by MTT assay. Antiproliferative activity against human ZR-75-1 cells incubated for 48 hrs assessed as reduction in cell viability by MTT assay.	42593900
ZR-75-1	IC50	1935 nM	Antiproliferative activity against human ZR-75-1 cells incubated for 72 hrs assessed as reduction in cell viability by MTT assay. Antiproliferative activity against human ZR-75-1 cells incubated for 72 hrs assessed as reduction in cell viability by MTT assay.	42593900

In Vitro

ZJC-11 (1 μM; 4 h) selectively binds to endogenous CDK7 in MDA-MB-231 cells and enhances the thermal stability of CDK7 compared with CDK1, CDK2 and CDK9^[1].
ZJC-11 (0-10000 nM; 24-72 h) potently inhibits the proliferation of triple-negative breast cancer cell lines (MDA-MB-231, CAL-148, MDA-MB-468, BT-549, MFM223), with IC₅₀ values ranging from 0.306 to 2.41 μM. It shows weak activity against the estrogen receptor-positive (ER+) breast cancer cell line ZR-75-1, and exhibits extremely low toxicity toward normal cell lines MCF10A and RAW264.7^[1].
ZJC-11 (0-500 nM; 14 days) inhibits colony formation of MDA-MB-231 and MDA-MB-468 cells in a dose-dependent manner, but exerts almost no effect on ZR-75-1 ER⁺ breast cancer cells^[1].
ZJC-11 (0-500 nM; 48 h) dose-dependently increases the proportion of dead cells in MDA-MB-231 and MDA-MB-468 cells^[1].
ZJC-11 (0-1000 nM; 6-48 h) dose-dependently inhibits the phosphorylation of Ser2, Ser5 and Ser7 sites on RNAPII CTD in MDA-MB-231 and MDA-MB-468 cells^[1].
ZJC-11 (0-500 nM; 48 h) induces DNA damage-driven therapy-induced senescence and senescence-associated secretory phenotype in MDA-MB-231 and MDA-MB-468 cells^[1].
ZJC-11 (0-1000 nM; 48 h) induces G2/M cell cycle arrest in MDA-MB-231 and MDA-MB-468 cells by downregulating cyclin B1 and phosphorylated CDK1^[1].
ZJC-11 (500 nM; 1 h pre-incubation, 12 h DOX incubation) alleviates DOX (HY-15142A)-induced cardiotoxicity in H9c2 and HL-1 cardiomyocytes by preserving mitochondrial function, reducing apoptosis, and restoring p-CDK1 levels^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-231, CAL-148, MDA-MB-468, BT-549, MFM223, ZR-75-1, MCF10A, RAW264.7, HepG2, JHH7, H446, HT29 cells
Concentration:

0, 10, 100, 1000, 10000 nM
Incubation Time:

48 h; 72 h; 24 h
Result:

Exhibited potent antiproliferative activity against TNBC cell lines, with IC₅₀ values of 0.60 μM for MDA-MB-231, 2.41 μM for CAL-148, 627.9 nM for MDA-MB-231 (48 h), 540.0 nM for MDA-MB-231 (72 h), 634.7 nM for MDA-MB-468 (48 h), and 305.7 nM for MDA-MB-468 (72 h).
Inhibited proliferation of BT-549, MFM223, HepG2, JHH7, H446, and HT29 cells.
Showed weaker activity against ER+ breast cancer ZR-75-1 cells, with IC₅₀ values of 2177 nM (48 h) and 1935 nM (72 h).
Reduced viability by 20-40% in normal MCF10A and RAW264.7 cells at 1 μM after 24 or 48 h.

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-231, MDA-MB-468, ZR-75-1 cells
Concentration:

0, 125, 250, 500 nM
Incubation Time:

14 days
Result:

Dose-dependently reduced the number of colonies formed by MDA-MB-231 and MDA-MB-468 TNBC cells, with near-complete inhibition at 500 nM.
Had only a minimal effect on colony formation by ZR-75-1 cells.

Cell Cytotoxicity Assay^[1]

Cell Line:

MDA-MB-231, MDA-MB-468, ZR-75-1 cells
Concentration:

0, 125, 250, 500 nM
Incubation Time:

48 h
Result:

Dose-dependently increased the dead-to-live cell ratio in MDA-MB-231 and MDA-MB-468 TNBC cells, with the ratio reaching ~15% and ~20% of control at 500 nM, respectively.
Had a negligible effect on the dead-to-live cell ratio in ZR-75-1 cells.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231, MDA-MB-468, ZR-75-1 cells
Concentration:

0, 125, 250, 500, 1000 nM
Incubation Time:

6 h; 24 h; 48 h
Result:

Dose-dependently reduced phosphorylation of RNAPII at Ser2, Ser5, and Ser7 sites in MDA-MB-231 and MDA-MB-468 TNBC cells, with more pronounced inhibition observed at longer incubation times.
Exerted a weaker inhibitory effect on RNAPII phosphorylation in ZR-75-1 ER+ breast cancer cells.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-231, MDA-MB-468, ZR-75-1 cells
Concentration:

0, 125, 250, 500, 1000 nM
Incubation Time:

48 h
Result:

Induced a significant increase in the proportion of G2/M phase cells and a decrease in S phase cells in MDA-MB-231 and MDA-MB-468 TNBC cells.
Dose-dependently reduced protein levels of cyclin B1 and p-CDK1 in these TNBC cell lines.
Had minimal effect on cell cycle distribution or cyclin B1/p-CDK1 levels in ZR-75-1 cells.
Downregulated G2/M phase-related genes in ZJC-11-treated MDA-MB-231 cells via RNA-seq analysis.

In Vivo

ZJC-11 (4-8 mg/kg, i.p., twice daily for 21 consecutive days) exhibits dose-dependent anti-triple-negative breast cancer activity in mice^[1].

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

Animal Model:

BALB/c-nu (female, 5 weeks old, triple-negative breast cancer model via MDA-MB-231 cell injection into fourth pair of mammary pads)^[1]
Dosage:

4 mg/kg; 8 mg/kg
Administration:

i.p.; twice daily; 21 days
Result:

Showed no obvious effect on mouse body weight compared to solvent-treated controls.
Exerted a dose-dependent inhibitory effect on tumor growth, with tumor growth inhibition (TGI) values of 73.09% at 8 mg/kg and 60.61% at 4 mg/kg.
Significantly reduced the tumor proliferation marker Ki67.
Showed no significant toxic effects on heart, liver, spleen, lung, or kidney via H&E staining.

Chemical Information

분자량 542.03
화학식 C₂₉H₂₈ClN₇O₂
SMILES

CN(C/C=C/C(NC1=CC(C(NC2=CC=CC(NC3=NC=C(C(NC4=CC=CC=C4)=N3)Cl)=C2)=O)=CC=C1)=O)C
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Chen B, et al. Discovery of ZJC-11 as a Novel Selective CDK7 Inhibitor for Treating Triple-Negative Breast Cancer by Inducing Cell Senescence. Journal of medicinal chemistry. 2026 Aug 13;69(15):18364-18385.

Calculators

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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