2. Cell Cycle/DNA Damage Apoptosis PI3K/Akt/mTOR
  3. CDK Apoptosis DNA/RNA Synthesis Akt
  4. YJZ5118

YJZ5118 is a selective CDK12/CDK13 inhibitor with IC50 values of 39.5 nM and 26.4 nM. YJZ5118 suppresses transcription of DNA damage response genes and induces DNA damage in tumor cells. YJZ5118 inhibits proliferation and triggers apoptosis. YJZ5118 inhibits RNA polymerase II Ser2 phosphorylation and increases Akt pathway activity. YJZ5118 exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for the research of cancer, such as prostate cancer.

For research use only. We do not sell to patients.

YJZ5118

YJZ5118 Chemical Structure

CAS No. : 3031861-18-1

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YJZ5118 Related Antibodies

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

YJZ5118 is a selective CDK12/CDK13 inhibitor with IC50 values of 39.5 nM and 26.4 nM. YJZ5118 suppresses transcription of DNA damage response genes and induces DNA damage in tumor cells. YJZ5118 inhibits proliferation and triggers apoptosis. YJZ5118 inhibits RNA polymerase II Ser2 phosphorylation and increases Akt pathway activity. YJZ5118 exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for the research of cancer, such as prostate cancer[1].

IC50 & Target[1]

RNA Polymerase

 

CDK12

39.5 nM (IC50)

CDK13

26.4 nM (IC50)

In Vitro

YJZ5118 is a potent, selective inhibitor of recombinant CDK12/Cyclin K and CDK13/Cyclin K with IC50 values of 39.5 nM and 26.4 nM, respectively, and over 100-fold selectivity relative to most other CDK family members[1].
YJZ5118 (0.1 μM; 2 h) acts as an irreversible inhibitor in VCaP prostate cancer cells, maintaining suppression of RNA polymerase II Ser2 phosphorylation, DDR gene expression, and antiproliferative activity after compound washout[1].
YJZ5118 (5 days) potently inhibits VCaP prostate cancer cell proliferation with an IC50 of 23.7 nM, and shows preferential activity against multiple cancer cell lines including prostate, breast, and Ewing's sarcoma cells, while normal/non-neoplastic cells are less sensitive[1].
YJZ5118 (20-100 nM; 1-48 h) inhibits RNA polymerase II Ser2 phosphorylation, suppresses transcription of long DDR genes, induces DNA damage, and triggers apoptosis in VCaP prostate cancer cells at concentrations as low as 100 nM[1].
YJZ5118 (10-100 nM; 24 h) dose-dependently activates the Akt pathway in VCaP prostate cancer cells, and exhibits synergistic antiproliferative effects with multiple Akt inhibitors in 22RV1 prostate cancer cells[1].

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

YJZ5118 Related Antibodies

Western Blot Analysis[1]

Cell Line: VCaP
cells
Concentration: 20, 50, 100 nM
Incubation Time: 1, 2, 4, 6, 8, 15, 24 h
Result: Reduced RNA polymerase II Ser2 phosphorylation levels.

Western Blot Analysis[1]

Cell Line: VCaP
cells
Concentration: 10, 20, 50, 100 nM
Incubation Time: 24 h
Result: Increased p-AKT and pPRAS40 levels.
Increased cPARP and γH2Ax levels.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t F CL
Mice[1] 2.5 mg/kg i.v. 1.29 h 0.08 h 2813.3 ng/mL 1575.0 ng/L.h / 28.34 mL/min/kg
Mice[1] 10 mg/kg p.o. 2.32 h 1.50 h 638.7 ng/mL 2235.5 ng·h/mL 35.53 % /
In Vivo

YJZ5118 (0.5-1.5 mg/kg; i.p.; daily; 27 days) significantly suppresses tumor growth in an orthotopic VCaP CRPC xenograft model, inhibits RNA polymerase II Ser2 phosphorylation, reduces DDR gene expression, and increases Akt pathway activity in tumors[1].

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

Animal Model: NSG; CB17SCID (female, 6-8 weeks old, orthotopic VCaP CRPC xenograft model)[1]
Dosage: 0.5 mg/kg; 1.5 mg/kg
Administration: i.p.; daily; 27 days
Result: Significantly reduced tumor volume compared to vehicle control.
Significantly lowered tumor weight compared to vehicle controls.
Inhibited phosphorylation of RNA polymerase II at Serine 2.
Increased levels of pAkt (S473) and pPRAS40 in tumors.
Reduced mRNA expression of DDR genes (ATM, ATR, BRCA1).
Did not alter CDK12 gene expression.
Increased pAkt levels and enhanced apoptosis in tumor sections (histological analysis).
Caused no significant changes in animal body weights.
Molecular Weight

620.79

Formula

C36H44N8O2
CAS No.
SMILES

C=CC(NC1=CC(N(C(NCC2=CC=CC=C2)=O)[C@H]3CC[C@@H](CC3)NC4=NC=C(C=C4)C#N)=CC=C1N5CCC(CC5)N(C)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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YJZ5118 Related Classifications

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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:

YJZ51183031861-18-1YJZ 5118YJZ-5118CDKApoptosisDNA/RNA SynthesisAktCyclin dependent kinasePKBProtein kinase Bewing’s sarcomaapoptosisbreast cancerCDK13prostate cancer cellscastration-resistant prostate cancerDNA damage response genesCDK12Akt inhibitorsDNA damageInhibitorinhibitorinhibit

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