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

CDK6/PIM1-IN-1 是一种有效且平衡的双重 CDK6/PIM1 抑制剂，IC50 分别为 39 nM 和 88 nM。CDK6/PIM1-IN-1 抑制 CDK4 (IC50=3.6 nM)。CDK6/PIM1-IN-1 可显著抑制急性髓系白血病 (AML) 细胞增殖，将细胞周期阻滞在 G1 期，并促进细胞凋亡。CDK6/PIM1-IN-1 具有抗AML活性。

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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 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

查看 Pim 亚型特异性产品:

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PIM1 PIM2 PIM3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

PIM1

88 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)

PIM2

>10 μM (IC50)

PIM3

92 nM (IC50)

细胞效力
(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]
体外研究
(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].

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

CDK6/PIM1-IN-1 相关抗体:
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

473.55

Formula

C25H28FN9
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CDK6/PIM1-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

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

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