P18IN011
P18IN011 is an inhibitor that specifically targets the interaction between p18(INK4C) and CDK6, with an IC50 of 3.61 μM against mouse p18INK4C. P18IN011 relieves p18-mediated CDK6 inhibition, thereby effectively regulating the G1 phase cell cycle checkpoint. P18IN011 significantly enhances the proliferation, self-renewal and bone marrow reconstitution abilities of hematopoietic stem cells, and increases the frequency of primitive hematopoietic cells to promote cobblestone area formation. Acting specifically on p18-expressing hematopoietic cells via CDK4/6, P18IN011 not only supports the ex vivo expansion of human umbilical cord blood hematopoietic stem cells, but also maintains their long-term reconstitution capacity during in vitro culture to enable multi-lineage transplantation.
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- CAS No.: 77408-67-4
- 화학식: C15H12N2O5S
- 분자량:332.33
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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CDK4 |
CDK6 |
P18IN011 (0.5 μM; 30 min) specifically blocks the inhibitory effect of p18 (but not p16) on CDK6 activity in vitro[2].
P18IN011 (20 μM; medium changed weekly; 8 weeks) maintains functional hematopoietic stem cell (HSC) activity during long-term in vitro culture[2].
P18IN011 (10 μM; 3 days) enhances the in vitro expansion of functional hematopoietic stem cells (HSCs)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The engraftment rate of primary transplantation for functional hematopoietic stem cells (HSC) treated with P18IN011 (10 μM; 3 d) reaches twice that of cells treated with P18IN003, while the frequency of functional HSC is 4.2-fold higher than that of the DMSO control group[2].
P18IN011 increases the frequency of primitive hematopoietic cells in ex vivo culture and significantly enhances the long-term reconstitution capacity of hematopoietic stem cells (HSCs) in immunodeficient mice, with stronger activity than P18IN003 (HY-123535)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (CD45.1 or CD45.2); B6.SJL-Ptprca Pep3b/Boy (CD45.1) (donor: 3-6-month-old male; recipient: 2-3-month-old female)[2]
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Dosage:/
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Administration:HSC transplantation
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Result:Produced significantly higher cobblestone area yields than controls and P18IN003 at the same concentration.
Showed no significant difference in colony-forming unit counts versus controls.
Achieved 22.06% long-term repopulation in all eight recipient mice, whereas no engraftment occurred in control groups.
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Animal Model:B6.SJL-Ptprca Pep3b/Boy (CD45.1); C57BL/6J (CD45.2) (recipient: 2-3-month-old female)[2]
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Dosage:/
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Administration:HSC transplantation
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Result:Increased primary transplantation engraftment levels (CD45.1+ cells) significantly versus DMSO controls and to levels two times higher than P18IN003-treated groups.
Achieved approximately 4.2-fold higher functional HSC frequency than DMSO controls.
Produced significantly higher frequency of CD45.1+ LKS cells than controls and 1.3-fold higher than P18IN003-treated groups.
Showed no significant differences in cell cycle phase distribution or apoptotic fractions versus controls.
Maintained significantly higher secondary transplantation engraftment levels than controls and higher levels than P18IN003-treated groups.
Chemical Information
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CAS No. 77408-67-4
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분자량 332.33
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화학식 C15H12N2O5S
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SMILES
O=C(NC1=CC=C(C=C1)S(=O)(=O)OC2=NOC=3C=CC=CC23)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[2]. Gao Y, et al. Small-molecule inhibitors targeting INK4 protein p18(INK4C) enhance ex vivo expansion of haematopoietic stem cells. Nature communications. 2015 Feb 18;6:6328. [Content Brief]
[3]. Zhang Y, et al. Novel chemical attempts at ex vivo hematopoietic stem cell expansion. International journal of hematology. 2016 May;103(5):519-29. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
P18IN011 Related Classifications
HY-102088 Related Classifications
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