2. Cell Cycle/DNA Damage
  3. CDK
  4. THZ1

THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.

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CAS 番号 : 1604810-83-4

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10 mM * 1 mL in DMSO
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10 mg $185 在庫あり
25 mg $350 在庫あり
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カスタマーレビュー

Based on 93 publication(s) in Google Scholar

Other Forms of THZ1:

THZ1 関連抗体

Top Publications Citing Use of Products

顧客検証

WB

    THZ1 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Jun;40(6):814-822.  [Abstract]

    The protein expression levels of the genes related to cell cycle and metabolism are detected by immunoblotting using the corresponding antibodies in H1299 cells treated with 20 nM THZ1 alone or in combination with 500 nM CB-839 for 48 h.

    THZ1 purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 May;38(20):3932-3945.  [Abstract]

    Immunoblot analysis of the MYC and β-actin in cells (MiaPaCa2 and MiaPaCa2-R) treated with the indicated dose of THZ1 for 6 h.

    THZ1 purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2019 Mar 22:12:2137-2147.  [Abstract]

    Western blot is used to assess the RNA Pol II protein and its phosphorylation at serine 2, serine 5, and serine 7 in cervical cancer cells after treatment with the indicated concentrations of THZ1.

    THZ1 purchased from MedChemExpress. Usage Cited in: Cell. 2018 Sep 20;175(1):171-185.e25.  [Abstract]

    WB analysis of MV4-11 cells treated with BTX161 (6 hr), iCDK9 (4 hr), or THZ1 (4 hr) at the indicated concentrations in different combinations as indicated. PP2Ac is a loading control.

    THZ1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Aug 23;9(1):3392.  [Abstract]

    21mers are synthesized in parallel reactions with unlabeled (upper panel) or radiolabeled (lower panel) ribonucleoside triphosphates in the presence of DMSO (-) or increasing amounts of THZ1; reactions are stopped after 15 or 60 min.

    THZ1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Nov 19;9(1):4866.  [Abstract]

    MYCN, PHOX2B, and TBX2 protein levels 10 h and 16 h upon treatment with 1 μM JQ1, 35 nM THZ1 and the combination of JQ1 and THZ1 in the IMR-5/75 cell line.

    THZ1 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2017 May 15;6(5):e336.  [Abstract]

    Lysates from cells treated with vehicle or 200 nM THZ1 for 48 h analyzed for the activation status of multiple CDKs as indicated to the right of panels by western blotting.

    THZ1 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Sep;16(9):1739-1750.  [Abstract]

    Western blot analysis of RNAPII CTD phosphorylation in ovarian cancer cells that are treated with THZ1.

    THZ1 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Sep;16(9):1739-1750.  [Abstract]

    Western blot analysis of RNAPII CTD phosphorylation in ovarian cancer cells that are treated with THZ1.

    THZ1 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Sep;16(9):1739-1750.  [Abstract]

    Western blot analysis of RNAPII CTD phosphorylation in ovarian cancer cells that are treated with THZ1.

    THZ1 purchased from MedChemExpress. Usage Cited in: TUMOR, 2017, 37(11): 1119-1127.

    The expression level of cyclin-dependent kinase 7 (CDK7) and the phosphorylation level of RNA polymeraseⅡ carboxyl-terminal domain Ser-5 (RNAPolⅡS5) in ovarian cancer cells treated with THZ1 are detected by Western blotting. After the ovarian cancer IGROV1, OVCA433, SKOV3 and COV413B cells are treated with 0.5 μM THZ1 for 0, 4, 8, 12 and 24 h, the CDK7 expression and RNAPolⅡS5 phosphorylation levels are significantly down-regulated.

    THZ1 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Apr 18;8(16):27353-27363.  [Abstract]

    Representative Western blot showing the phosphorylation status of ERα at serine 118 (S118) in MCF-7 cells in controls and after treatment with the CDK7 inhibitor, THZ1 (100 nM), or AG-490 (100 μM) for 3 h prior to E2 treatment for 30 min. Endogenous ERα and β-actin are used as loading controls.

    CDK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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    製品説明

    THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression[1][2].

    IC50 & Target[1][2]

    CDK7

    3.2 nM (IC50)

    CDK12

     

    CDK13

     

    Cellular Effect
    Cell Line Type Value Description References
    HL-60 EC50
    38 1
    Compound: THZ1
    Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay
    		[PMID: 31477350]
    HL-60 EC50
    38 1
    Compound: THZ1
    Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay
    		[PMID: 31477350]
    HL-60 EC50
    38 1
    Compound: THZ1
    Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay
    		[PMID: 31477350]
    Jurkat IC50
    50 1
    Compound: THZI
    Cytotoxicity against human Jurkat cells assessed as cell viability after 72 hrs by resazurin assay
    Cytotoxicity against human Jurkat cells assessed as cell viability after 72 hrs by resazurin assay
    		[PMID: 26115571]
    KOPTK1 IC50
    0.001 3
    Compound: 23; THZ1
    Cytotoxicity against human KOPTK1 cells assessed as reduction in cell viability
    Cytotoxicity against human KOPTK1 cells assessed as reduction in cell viability
    		[PMID: 31514062]
    THP-1 IC50
    77 3
    Compound: 1; THZ1
    Cytotoxicity against human THP-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
    Cytotoxicity against human THP-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
    		[PMID: 36384292]
    Jurkat IC50
    50 1
    Compound: THZI
    Cytotoxicity against human Jurkat cells assessed as cell viability after 72 hrs by resazurin assay
    Cytotoxicity against human Jurkat cells assessed as cell viability after 72 hrs by resazurin assay
    		[PMID: 26115571]
    THP-1 IC50
    77 3
    Compound: 1; THZ1
    Cytotoxicity against human THP-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
    Cytotoxicity against human THP-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
    		[PMID: 36384292]
    Jurkat IC50
    50 1
    Compound: THZI
    Cytotoxicity against human Jurkat cells assessed as cell viability after 72 hrs by resazurin assay
    Cytotoxicity against human Jurkat cells assessed as cell viability after 72 hrs by resazurin assay
    		[PMID: 26115571]
    KOPTK1 IC50
    0.001 3
    Compound: 23; THZ1
    Cytotoxicity against human KOPTK1 cells assessed as reduction in cell viability
    Cytotoxicity against human KOPTK1 cells assessed as reduction in cell viability
    		[PMID: 31514062]
    MV4-11 IC50
    30.7 1
    Compound: THZ1
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    		[PMID: 39140066]
    THP-1 IC50
    77 3
    Compound: 1; THZ1
    Cytotoxicity against human THP-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
    Cytotoxicity against human THP-1 cells assessed as cell viability measured after 24 hrs by CCK-8 assay
    		[PMID: 36384292]
    体外実験

    THZ1 inhibits Jurkat cell and Loucy cell with IC50 of 50 nM, and 0.55 nM, respectively. THZ1 (9, 27, 83, 250, 750, and 2500 nM) inhibits CDK12 but at higher concentrations compared to CDK7. THZ1 (1 μM) irreversibly inhibits RNAPII CTD and CAK phosphorylation. THZ1 (2.5 μM) irreversibly inhibits RNAPII CTD phosphorylation by covalently targeting a unique cysteine located outside the kinase domain of CDK7 in Hela S3 cells. THZ1 (250 nM) causes decreased cellular proliferation and an increase in apoptotic index with concomitant reduction in anti-apoptotic proteins, most notably MCL-1 and XIAP in T-ALL cell lines[1].
    All genotypically-distinct human (hSCLC) cell lines exhibit high sensitivity to THZ1, with an IC50 in the range of 5-20 nM[3].

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

    THZ1 関連抗体
    体内実験

    THZ1 (10 mg/kg) demonstrates potent killing of primary chronic lymphocytic leukemia (CLL) cells and anti-proliferative activity against primary TALL cells and in vivo against a human T-ALL xenograft[1].
    THZ1 (10 mg/kg, i.v.) inhibits tumor growth in a mouse model of human MYCN-amplified NB and shows no toxicity[4].
    THZ1 (10 mg/kg, i.p.) completely suppresses oesophageal squamous cell carcinoma tumour growth in vivo without loss of body weight or other common toxic effects[5].

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

    566.05

    分子式

    C31H28ClN7O2
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    ClC1=CN=C(NC2=CC(NC(C3=CC=C(NC(/C=C/CN(C)C)=O)C=C3)=O)=CC=C2)N=C1C4=CNC5=CC=CC=C54
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (176.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7666 mL 8.8331 mL 17.6663 mL
    5 mM 0.3533 mL 1.7666 mL 3.5333 mL
    10 mM 0.1767 mL 0.8833 mL 1.7666 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

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    体積 （終了）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Saline

      Solubility: 5 mg/mL (8.83 mM); Suspended solution; Need ultrasonic

    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (17.67 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.84%

    COA (258 KB) LCMS (112 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [1]

    Jurkat, Loucy, KOPTK1, and DND-41 cell lines are seeded in 384-well microplates at 15% confluency in medium. Cells are treated with THZ1 (2, 10, 50, 250, 1250, and 6250 nM) or DMSO for 72 hrs and cell viability is determined using resazurin[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Mice[1]
    Thirty-two NOD-SCIDIL2Rcγnull (NSG) 9-week old female mice are divided into treatment groups based on mean BLI as follows: THZ1 10 mg/kg qD, THZ1 10 mg/kg BID, and vehicle (10% DMSO in D5W) BID (n=10 for all groups). Two mice are excluded, one with the highest and one with the lowest BLI. All treatments are administered via IV injection in the lateral tail vein in a volume of 3.3 μL/g (non-blinded). Mice are imaged and weighed every 3-5 days. Mice are treated for four weeks and on the final day mice are imaged, dosed and sacrificed approximately 5-6 hrs post dose. Upon sacrifice, blood is collected via cardiac puncture in EDTA tubes; a portion (300 uL) is processed for plasma. Liver and spleen tissues are collected from each mouse with half of each sample flash frozen and half of each sample fixed. Blood plasma and liver samples are processed for pharmacokinetics analysis of THZ1. Spleen tissues are homogenized and lysed and processed for pharmacodynamics analysis of THZ1 target engagement.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7666 mL 8.8331 mL 17.6663 mL 44.1657 mL
    5 mM 0.3533 mL 1.7666 mL 3.5333 mL 8.8331 mL
    10 mM 0.1767 mL 0.8833 mL 1.7666 mL 4.4166 mL
    15 mM 0.1178 mL 0.5889 mL 1.1778 mL 2.9444 mL
    20 mM 0.0883 mL 0.4417 mL 0.8833 mL 2.2083 mL
    25 mM 0.0707 mL 0.3533 mL 0.7067 mL 1.7666 mL
    30 mM 0.0589 mL 0.2944 mL 0.5889 mL 1.4722 mL
    40 mM 0.0442 mL 0.2208 mL 0.4417 mL 1.1041 mL
    50 mM 0.0353 mL 0.1767 mL 0.3533 mL 0.8833 mL
    60 mM 0.0294 mL 0.1472 mL 0.2944 mL 0.7361 mL
    80 mM 0.0221 mL 0.1104 mL 0.2208 mL 0.5521 mL
    100 mM 0.0177 mL 0.0883 mL 0.1767 mL 0.4417 mL
    • No file chosen (Maximum size is: 1024 Kb)
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    THZ1 Related Classifications

    • Molarity Calculator

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    THZ11604810-83-4THZ 1THZ-1CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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