2. Cell Cycle/DNA Damage JAK/STAT Signaling Apoptosis
  3. CDK Pim Apoptosis
  4. CDK6/PIM1-IN-1

CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity.

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CDK6/PIM1-IN-1 Chemical Structure

CDK6/PIM1-IN-1 Chemical Structure

CAS No. : 2677026-14-9

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CDK6/PIM1-IN-1 Related Antibodies

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Description

CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity[1].

IC50 & Target[1]

CDK6/cyclinD1

39 nM (IC50)

CDK1/cyclinB

>10 μM (IC50)

CDK2/cyclinA

2.274 μM (IC50)

CDK3/Cyclin E

>10 μM (IC50)

Cdk4/cyclin D1

3.6 nM (IC50)

Cdk5/p25

>10 μM (IC50)

CDK7/Cyclin H/MNAT1

393 nM (IC50)

CDK9/cyclinT1

440 nM (IC50)

CDK12/Cyclin K

>10 μM (IC50)

CDK13/Cyclin K

>10 μM (IC50)

PIM1

88 nM (IC50)

PIM2

>10 μM (IC50)

PIM3

92 nM (IC50)

In Vitro

CDK6/PIM1-IN-1 (compound 51) exhibits more than 10 times selectivity over CDK1 (IC50>10 μM), CDK2 (IC50=2.274 μM), CDK3 (IC50>10 μM), CDK5 (IC50>10 μM), CDK7 (IC50=393 nM), CDK9 (IC50=440 nM), CDK12 (IC50>10 μM), and CDK13 (IC50>10 μM). CDK6/PIM1-IN-1 shows inhibitory activity against PIM2 (IC50>10 μM) and PIM3 (IC50=92 nM)[1].
CDK6/PIM1-IN-1 inhibits proliferation in AML cells (K562 cell,GI50=1.026 μM; HL-60 cell,GI50=1.069 μM; MOLM13 cell, GI50=1.362 μM)[1].
CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM) causes a G1 arrest in a dose-dependent manner in K562 and HL-60 cell lines[1].
CDK6/PIM1-IN-1 (1, 2, 4 μM) promotes the apoptosis of K562 and HL-60 cell lines in a dose-dependent manner[1].
CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM; for 24 h) reduces p-retinoblastoma (RB) and p-BAD levels in a concentration-dependent manner. CDK6/PIM1-IN-1 decreases the PIM1 level[1].

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

CDK6/PIM1-IN-1 Related Antibodies
In Vivo

CDK6/PIM1-IN-1 (compound 51; orally; 60, 90 mg/kg/day; 17 days) displays more potent antitumor activity in BALB/c mice with K562 cell lines[1].
CDK6/PIM1-IN-1 (iv; 5 mg/kg) has the t1/2, MRT0-∞, and AUC0-∞ values of 9.78 h, 14.61 h, and 1153.74 h·ng/mL, respectively in Sprague–Dawley (SD) rats[1].
CDK6/PIM1-IN-1 (po; 5 mg/kg) has the t1/2, Tmax, Cmax, and AUC0-∞ of 15.81 h, 11 h, 152.31 ng/mL, and 5152.92 h·ng/mL, respectively in SD rats[1].

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

473.55

Formula

C25H28FN9
CAS No.
SMILES

FC1=CN=C(NC2=NC=C(N3CCNCC3)C=C2)N=C1C4=CC=C5N=CC(N(CC)CC)=NC5=C4
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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CDK6/PIM1-IN-1 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:

CDK6/PIM1-IN-12677026-14-9CDKPimApoptosisCyclin dependent kinasePim kinasesacute myeloid leukemiaAMLG1 phase,?K562HL-60MOLM13 cellInhibitorinhibitorinhibit

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