2. Cell Cycle/DNA Damage Apoptosis Epigenetics
  3. CDK Apoptosis DNA/RNA Synthesis Aurora Kinase
  4. LS-Q2

LS-Q2 is a highly selective CDK4/9 inhibitor with IC50 values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.

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

LS-Q2

LS-Q2 Chemical Structure

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LS-Q2 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 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Aurora Kinase Aurora A Aurora B Aurora C

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Description

LS-Q2 is a highly selective CDK4/9 inhibitor with IC50 values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors[1].

IC50 & Target[1]

CDK4

1.4 nM (IC50)

CDK9

6.2 nM (IC50)

CDK6

52 nM (IC50)

Aurora A

212 nM (IC50)

CDK7

748 nM (IC50)

CDK5

795 nM (IC50)

CDK1

1249 nM (IC50)

CDK2

1491 nM (IC50)

CDK8

>10000 nM (IC50)

In Vitro

LS-Q2 (Compound 6m) shows potent inhibitory activity against CDK4 and 9 with IC50 values of 1.4 and 6.2 nM, and shows weak inhibitory against CDK6 (IC50 = 52 nM), CDK1, 2, 5, 7, 8 (IC50 >700 nM)[1].
LS-Q2 inhibits tumor cell proliferation with in MIA Paca-2, HCT116, Hela cells with IC50 values of 0.62, 0.75, 2.77 μM[1].
LS-Q2 (0.5-2 μM; 24 h) induces G2/M phase arrest and apoptosis in HepG2 cells[1].
LS-Q2 (0.5-2 μM; 24 h) reduces pSer2 RNA polymerase II expression in HepG2 cells[1].

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

LS-Q2 Related Antibodies

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Reduced pSer2 RNA polymerase II, P-RB expression.
Parmacokinetics
Species Dose Route AUC0-t MRT0-t T1/2β Tmax Cmax Vz CL F
Mice[1] 5 mg/kg i.v. 1376 ng·h/mL 3.16 h 6.49 h 0.03 h 1903 ng/mL 32812 mL/kg 3535 mL/h/kg /
Mice[1] 25 mg/kg p.o. 2758 ng·h/mL 3.38 h 4.60 h 0.65 h 1205 ng/mL 57823 mL/kg 9074 mL/h/kg 40.1 %
Molecular Weight

461.60

Formula

C26H35N7O
SMILES

CN(C(C1=CC2=C(N1C3CCCC3)N=C(N=C2)NC4=CC=C(C=C4)CN5CCCNCC5)=O)C
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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LS-Q2 Related Classifications

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× = ×
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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:

LS-Q2CDKApoptosisDNA/RNA SynthesisAurora KinaseCyclin dependent kinaseCDK9Bcl-2 inhibitorstumor cellsCDK4malignant solid tumorsBET inhibitorsInhibitorinhibitorinhibit

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