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)

Cellular Effect
Cell Line Type Value Description References
HL-60 GI50
1.07 μM
Compound: 51
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34958208]
K562 GI50
1.03 μM
Compound: 51
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 34958208]
MOLM-13 GI50
1.362 μM
Compound: 51
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34958208]
Mononuclear cell line GI50
5.33 μM
Compound: 51
Antiproliferative activity against AML patient derived mononuclear cells of assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against AML patient derived mononuclear cells of assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
[PMID: 34958208]
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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