1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK9-IN-2

CDK9-IN-2 

Cat. No.: HY-16462 Purity: 99.84%
Handling Instructions

CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.

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

CDK9-IN-2 Chemical Structure

CDK9-IN-2 Chemical Structure

CAS No. : 1263369-28-3

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 264 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 960 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CDK9-IN-2 purchased from MCE. Usage Cited in: Cancer Discov. 2017 Mar;7(3):302-321.

    Small molecule inhibitor of CDK9, HY-16462, similarly blocks adaptive PDGFRB and DDR1 upregulation. Attenuation of 24 h 100 nM Trametinib-induced PDGFRB and DDR1 upregulation by co-treatment with 100 nM HY-16462.

    CDK9-IN-2 purchased from MCE. Usage Cited in: PLoS One. 2017 May 16;12(5):e0177871.

    Mcl-1 mRNA is similarly reduced. Immunoblot analysis revealed that the highest concentrations of CDK9 inhibitors strongly reduce Mcl-1 protein.
    • Biological Activity

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    Description

    CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.

    IC50 & Target

    IC50: 5 nM (CDK9, in H929 multiple myeloma cell line), 7 nM (CDK9, in A2058 skin cell line)[1]

    In Vitro

    CDK9-IN-2 (200 nM) reduces the expression of MEPCE indicating that MEPCE is a pharmacodynamic (PD) marker for any CDK9 inhibitor. The expression of MCL1 protein is reduced 2 hours after treatment and is further reduced after 16 hour exposure to CDK9-IN-2 (500 nM)[1].

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

    Molecular Weight

    425.93

    Formula

    C₂₃H₂₅ClFN₅

    CAS No.

    1263369-28-3

    SMILES

    ClC1=CN=C(N[[email protected]@H]2CC[[email protected]@H](N)CC2)C=C1C3=NC(NCC4=CC(F)=CC=C4)=CC=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (117.39 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3478 mL 11.7390 mL 23.4780 mL
    5 mM 0.4696 mL 2.3478 mL 4.6956 mL
    10 mM 0.2348 mL 1.1739 mL 2.3478 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    H929, A2058, A375, U87MG, and NCIH441 cell lines are treated with CDK9-IN-2 at 500 nM (high) or 200 nM (low) at different time points. Five cell lines are analyzed: NCI-H929, a multiple myeloma cell line; NCI-H441 , a lung papillary adenocarcinoma cell line; A375, a melanoma cell line; A2058, a melanoma cell line and U-87-MG, a glioblastoma cell line. Cell lines are grown in the medium recommended by ATCC and treated as follows: NCI-H929: 2 hours: DMSO, 200 nM CDK9-IN-2 or 500nM CDK9-IN-2. NCI-H441 and A375: 0 timepoint: Untreated, harvested when compound is added to the other plates. 2 hours: DMSO, 200 nM CDK9-IN-2 or 500 nM CDK9-IN-2 or 500 nM CKDI(7) (3 plates each, total 12 plates).8 hours: DMSO, 200 nM CDK9-IN-2 or 500 nM CDK9-IN-2 or 500 nM CKDI(7) (3 plates each, total 12 plates).16 hours: DMSO, 200 nM CDK9-IN-2 or 500 nM CDK9-IN-2 or 500 nM CKDI(7) (3 plates each, total 12 plates). A2058 and U-87-MG: 0 timepoint: Untreated, harvested when compound is added to the other plates (3 plates). 2 hours: DMSO, 500 nM CDK9-IN-2 (3 plates each, total 6 plates). 8 hours: DMSO, 500 nM CDK9-IN-2 (3 plates each, total 6 plates).16 hours: DMSO, 500 nM CDK9-IN-2 (3 plates each, total 6 plates). The IC50s arethe analysed[1].

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

    References
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    Keywords:

    CDK9-IN-2CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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    Product Name:
    CDK9-IN-2
    Cat. No.:
    HY-16462
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