THZ1 Hydrochloride
Based on 95 publication(s) in Google Scholar
THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.06%
- Formule: C31H29Cl2N7O2
- Masse moléculaire:602.51
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) THZ1 Hydrochloride
More- Nat Med. 2019 Feb;25(2):292-300. [Abstract]
- Science. 2021 Apr 30;372(6541):eaba8490. [Abstract]
- Cell. 2018 Sep 20;175(1):171-185.e25. [Abstract]
- Cell. 2017 Sep 7;170(6):1209-1223.e20. [Abstract]
- Cancer Discov. 2019 Nov;9(11):1538-1555. [Abstract]
- Nat Cell Biol. 2020 Oct;22(10):1187-1196. [Abstract]
- Cancer Res. 2025 May 14. [Abstract]
- Cancer Res. 2021 Jun 1;81(11):3105-3120. [Abstract]
- Autophagy. 2021 Jun;17(6):1426-1447. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Feb 2;16(1):1271. [Abstract]
- Nat Commun. 2024 Aug 9;15(1):6810. [Abstract]
- Nat Commun. 2019 Jul 25;10(1):3319. [Abstract]
- Nat Commun. 2018 Nov 19;9(1):4866. [Abstract]
- Nat Commun. 2018 Aug 23;9(1):3392. [Abstract]
- Hepatology. 2019 Jun;69(6):2502-2517. [Abstract]
- Mol Cell. 2026 Feb 19;86(4):674-692.e10. [Abstract]
- Mol Cell. 2019 May 16;74(4):674-687.e11. [Abstract]
- J Exp Clin Cancer Res. 2023 Aug 21;42(1):214. [Abstract]
- J Exp Clin Cancer Res. 2022 Oct 22;41(1):311. [Abstract]
- J Exp Clin Cancer Res. 2022 Aug 10;41(1):241. [Abstract]
- J Exp Clin Cancer Res. 2021 Apr 26;40(1):141. [Abstract]
- Cell Rep Med. 2023 Apr 18;4(4):101007. [Abstract]
- Sci Adv. 2020 Jul 17;6(29):eaba1593. [Abstract]
- Cell Death Differ. 2023 May;30(5):1260-1278. [Abstract]
- Cell Death Dis. 2021 Aug 3;12(8):763. [Abstract]
- Cell Death Dis. 2021 Mar 3;12(3):229. [Abstract]
- Cell Death Dis. 2020 Sep 15;11(9):754. [Abstract]
- Cell Death Dis. 2019 Aug 9;10(8):602. [Abstract]
- Cancer Lett. 2024 May 1:589:216811. [Abstract]
- Cancer Lett. 2021 Jun 1:507:70-79. [Abstract]
- Int J Biol Sci. 2019 Jun 10;15(8):1733-1742. [Abstract]
- Cell Commun Signal. 2022 Sep 5;20(1):96. [Abstract]
- Clin Cancer Res. 2019 Oct 15;25(20):6195-6205. [Abstract]
- Acta Pharmacol Sin. 2019 Jun;40(6):814-822. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. [Abstract]
- Chin Med J (Engl). 2022 Oct 20;135(20):2436-2445. [Abstract]
- Oncogene. 2022 Sep;41(40):4524-4536. [Abstract]
- Oncogene. 2019 May;38(20):3932-3945. [Abstract]
- Cell Chem Biol. 2025 Apr 17;32(4):556-569.e24. [Abstract]
- Regen Biomater. 2024 Mar 1:11:rbae020. [Abstract]
- EMBO Mol Med. 2022 Apr 7;14(4):e14990. [Abstract]
- Cancer Immunol Res. 2021 Jun;9(6):707-722. [Abstract]
- Cell Rep. 2022 Apr 26;39(4):110732. [Abstract]
- Br J Pharmacol. 2026 Jul 24.
- Genes Dev. 2020 Jan 1;34(1-2):53-71. [Abstract]
- J Med Chem. 2026 Aug 13;69(15):18364-18385.
- J Med Chem. 2022 Dec 8;65(23):15770-15788. [Abstract]
- J Invest Dermatol. 2021 Nov;141(11):2656-2667.e11. [Abstract]
- Mol Cancer Ther. 2025 Dec 4. [Abstract]
- Mol Cancer Ther. 2017 Sep;16(9):1739-1750. [Abstract]
- JCI Insight. 2026 Jan 15;11(4):e192113. [Abstract]
- Breast Cancer Res. 2023 May 5;25(1):51. [Abstract]
- Cells. 2021 May 12;10(5):1182. [Abstract]
- Oncogenesis. 2020 May 12;9(5):47. [Abstract]
- Cells. 2020 Mar 6;9(3):638. [Abstract]
- Cells. 2020 Mar 4;9(3):621. [Abstract]
- Cells. 2019 Oct 6;8(10):1208. [Abstract]
- Oncogenesis. 2017 May 15;6(5):e336. [Abstract]
- Eur J Pharmacol. 2023 Sep 15:955:175892. [Abstract]
- Cell Oncol (Dordr). 2021 Aug;44(4):871-887. [Abstract]
- mBio. 2025 Dec 10;16(12):e0289825. [Abstract]
- PLoS Pathog. 2025 Nov 11;21(11):e1013694. [Abstract]
- Sci Rep. 2024 May 8;14(1):10582. [Abstract]
- PLoS Pathog. 2024 Apr 19;20(4):e1012138. [Abstract]
- Cancers (Basel). 2022 Jun 1;14(11):2755. [Abstract]
- iScience. 2024 May 16;27(6):110011. [Abstract]
- Front Mol Biosci. 2021 Aug 19;8:697457. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2019 Jun;1866(6):978-991. [Abstract]
- Drug Dev Res. 2025 Feb;86(1):e70049. [Abstract]
- FEBS J. 2024 Oct;291(19):4240-4264. [Abstract]
- Front Oncol. 2021 May 24;11:664848. [Abstract]
- Front Oncol. 2021 Apr 6:11:663360. [Abstract]
- IUBMB Life. 2021 Dec;73(12):1446-1459. [Abstract]
- Biochem Biophys Res Commun. 2023 Dec 31:689:149188. [Abstract]
- J Mol Neurosci. 2022 Feb;72(2):410-419. [Abstract]
- Onco Targets Ther. 2019 Mar 22:12:2137-2147. [Abstract]
- Res Sq. 2025 Dec 18.
- bioRxiv. 2025 Aug 19.
- Res Sq. 2025 Apr 24:rs.3.rs-6506954. [Abstract]
- bioRxiv. 2024 July 27.
- bioRxiv. 2024 July 12.
- Heliyon. 2024 Jan 9;10(2):e24389. [Abstract]
- Research Square Print. September 29th, 2022.
- Patent. US20220288067A1.
- University of London. 2022 May.
- Research Square Print. 2022 May.
- Research Square Preprint. 2022 Feb.
- Research Square Preprint. 2022 Jan.
- Universidade de Lisboa. 2021 Dec 21.
- bioRxiv. June 18, 2021.
- bioRxiv. 2019 Oct.
- Oncotarget. 2017 Apr 18;8(16):27353-27363. [Abstract]
- TUMOR, 2017, 37(11): 1119-1127.
- Harvard Medical School LINCS LIBRARY
Customer Validation & Images
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Activité biologique
Description
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CDK7 3.2 nM (IC50) |
CDK12 |
CDK13 |
In Vitro
THZ1 inhibits Jurkat cell and Loucy cell with IC50 of 50 nM, and 0.55 nM, respectively. THZ1 demonstrates time-dependent inhibition of CDK7 in vitro and covalent binding of intracellular CDK7. 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].
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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.
In Vivo
? 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.
Chemical Information
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Appearance Solid
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Masse moléculaire 602.51
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Formule C31H29Cl2N7O2
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Color Yellow to brown
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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.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (95)
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Journal Impact Factor
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Most Recent
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Nat Med
2019 Feb;25(2):292-300. PMID: 30664779 -
Science
2021 Apr 30;372(6541):eaba8490. PMID: 33795473 -
Cell
Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. [Abstract]2018 Sep 20;175(1):171-185.e25. PMID: 30146162
THZ1 Hydrochloride 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.
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Cell
Excess Translation of Epigenetic Regulators Contributes to Fragile X Syndrome and Is Alleviated by Brd4 Inhibition. [Abstract]2017 Sep 7;170(6):1209-1223.e20. PMID: 28823556 -
Cancer Discov
CDK7 Inhibition Suppresses Castration-Resistant Prostate Cancer through MED1 Inactivation. [Abstract]2019 Nov;9(11):1538-1555. PMID: 31466944 -
Nat Cell Biol
2020 Oct;22(10):1187-1196. PMID: 32929202 -
Cancer Res
SMARCA4 loss increases RNA Polymerase II pausing and elevates R-loops to inhibit BRCA1-mediated repair in ovarian cancer. [Abstract]2025 May 14. PMID: 40366633 -
Cancer Res
Inhibition of the FACT Complex Targets Aberrant Hedgehog Signaling and Overcomes Resistance to Smoothened Antagonists. [Abstract]2021 Jun 1;81(11):3105-3120. PMID: 33853831 -
Autophagy
An integrative multi-omics approach uncovers the regulatory role of CDK7 and CDK4 in autophagy activation induced by silica nanoparticles. [Abstract]2021 Jun;17(6):1426-1447. PMID: 32397800 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
Nuclear ANLN regulates transcription initiation related Pol II clustering and target gene expression. [Abstract]2025 Feb 2;16(1):1271. PMID: 39894879 -
Nat Commun
Super enhancer acquisition drives expression of oncogenic PPP1R15B that regulates protein homeostasis in multiple myeloma. [Abstract]2024 Aug 9;15(1):6810. PMID: 39122682 -
Nat Commun
2019 Jul 25;10(1):3319. PMID: 31346162 -
Nat Commun
TBX2 is a neuroblastoma core regulatory circuitry component enhancing MYCN/FOXM1 reactivation of DREAM targets. [Abstract]2018 Nov 19;9(1):4866. PMID: 30451831
THZ1 Hydrochloride 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.
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Nat Commun
CTD-dependent and -independent mechanisms govern co-transcriptional capping of Pol II transcripts. [Abstract]2018 Aug 23;9(1):3392. PMID: 30139934
THZ1 Hydrochloride 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.
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Hepatology
2019 Jun;69(6):2502-2517. PMID: 30723918 -
Mol Cell
HSPA1A and DNAJB1 regulate NELF condensate dynamics to safeguard transcriptional recovery under heat stress. [Abstract]2026 Feb 19;86(4):674-692.e10. PMID: 41653920 -
Mol Cell
2019 May 16;74(4):674-687.e11. PMID: 30928206 -
J Exp Clin Cancer Res
MYC up-regulation confers vulnerability to dual inhibition of CDK12 and CDK13 in high-risk Group 3 medulloblastoma. [Abstract]2023 Aug 21;42(1):214. PMID: 37599362 -
J Exp Clin Cancer Res
Dissecting super-enhancer driven transcriptional dependencies reveals novel therapeutic strategies and targets for group 3 subtype medulloblastoma. [Abstract]2022 Oct 22;41(1):311. PMID: 36273157 -
J Exp Clin Cancer Res
2022 Aug 10;41(1):241. PMID: 35945614 -
J Exp Clin Cancer Res
Inhibition of retinoic acid receptor α phosphorylation represses the progression of triple-negative breast cancer via transactivating miR-3074-5p to target DHRS3. [Abstract]2021 Apr 26;40(1):141. PMID: 33902658 -
Cell Rep Med
USP9X mediates an acute adaptive response to MAPK suppression in pancreatic cancer but creates multiple actionable therapeutic vulnerabilities. [Abstract]2023 Apr 18;4(4):101007. PMID: 37030295 -
Sci Adv
β-Catenin safeguards the ground state of mousepluripotency by strengthening the robustness of the transcriptional apparatus. [Abstract]2020 Jul 17;6(29):eaba1593. PMID: 32832621 -
Cell Death Differ
BAP18 facilitates CTCF-mediated chromatin accessible to regulate enhancer activity in breast cancer. [Abstract]2023 May;30(5):1260-1278. PMID: 36828916 -
Cell Death Dis
Transcriptional CDK inhibitors, CYC065 and THZ1 promote Bim-dependent apoptosis in primary and recurrent GBM through cell cycle arrest and Mcl-1 downregulation. [Abstract]2021 Aug 3;12(8):763. PMID: 34344865 -
Cell Death Dis
2021 Mar 3;12(3):229. PMID: 33658484 -
Cell Death Dis
2020 Sep 15;11(9):754. PMID: 32934219 -
Cell Death Dis
CDK7 inhibitor THZ1 inhibits MCL1 synthesis and drives cholangiocarcinoma apoptosis in combination with BCL2/BCL-XL inhibitor ABT-263. [Abstract]2019 Aug 9;10(8):602. PMID: 31399555 -
Cancer Lett
Super-enhancer mediated upregulation of MYEOV suppresses ferroptosis in lung adenocarcinoma. [Abstract]2024 May 1:589:216811. PMID: 38490328 -
Cancer Lett
CDK7 inhibition by THZ1 suppresses cancer stemness in both chemonaïve and chemoresistant urothelial carcinoma via the hedgehog signaling pathway. [Abstract]2021 Jun 1:507:70-79. PMID: 33741425 -
Int J Biol Sci
Inhibition of super enhancer downregulates the expression of KLF5 in basal-like breast cancers. [Abstract]2019 Jun 10;15(8):1733-1742. PMID: 31360115 -
Cell Commun Signal
Elevation of effective p53 expression sensitizes wild-type p53 breast cancer cells to CDK7 inhibitor THZ1. [Abstract]2022 Sep 5;20(1):96. PMID: 36058938 -
Clin Cancer Res
The Covalent CDK7 Inhibitor THZ1 Potently Induces Apoptosis in Multiple Myeloma Cells In Vitro and In Vivo. [Abstract]2019 Oct 15;25(20):6195-6205. PMID: 31358538 -
Acta Pharmacol Sin
THZ1 suppresses human non-small-cell lung cancer cells in vitro through interference with cancer metabolism. [Abstract]2019 Jun;40(6):814-822. PMID: 30446732
THZ1 Hydrochloride 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.
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Proc Natl Acad Sci U S A
CDK7 inhibition suppresses aberrant hedgehog pathway and overcomes resistance to smoothened antagonists. [Abstract]2019 Jun 25;116(26):12986-12995. PMID: 31182587 -
Chin Med J (Engl)
Inhibition of MYC suppresses programmed cell death ligand-1 expression and enhances immunotherapy in triple-negative breast cancer. [Abstract]2022 Oct 20;135(20):2436-2445. PMID: 36583862 -
Oncogene
2022 Sep;41(40):4524-4536. PMID: 36042349 -
Oncogene
2019 May;38(20):3932-3945. PMID: 30692639
THZ1 Hydrochloride 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.
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Cell Chem Biol
CDK2 heterobifunctional degraders co-degrade CDK2 and cyclin E resulting in efficacy in CCNE1-amplified and overexpressed cancers. [Abstract]2025 Apr 17;32(4):556-569.e24. PMID: 40250405 -
Regen Biomater
Fabrication of a 3D bioprinting model for posterior capsule opacification using GelMA and PLMA hydrogel-coated resin. [Abstract]2024 Mar 1:11:rbae020. PMID: 38529352 -
EMBO Mol Med
CDK7/12/13 inhibition targets an oscillating leukemia stem cell network and synergizes with venetoclax in acute myeloid leukemia. [Abstract]2022 Apr 7;14(4):e14990. PMID: 35253392 -
Cancer Immunol Res
Targeting Triple-Negative Breast Cancer with Combination Therapy of EGFR CAR T Cells and CDK7 Inhibition. [Abstract]2021 Jun;9(6):707-722. PMID: 33875483 -
Cell Rep
RPAP2 regulates a transcription initiation checkpoint by inhibiting assembly of pre-initiation complex. [Abstract]2022 Apr 26;39(4):110732. PMID: 35476980 -
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Genes Dev
CDK7 regulates organ size and tumor growth by safeguarding the Hippo pathway effector Yki/Yap/Taz in the nucleus. [Abstract]2020 Jan 1;34(1-2):53-71. PMID: 31857346 -
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J Med Chem
Discovery of Novel N-(5-(Pyridin-3-yl)-1 H-indazol-3-yl)benzamide Derivatives as Potent Cyclin-Dependent Kinase 7 Inhibitors for the Treatment of Autosomal Dominant Polycystic Kidney Disease. [Abstract]2022 Dec 8;65(23):15770-15788. PMID: 36384292 -
J Invest Dermatol
Cyclin-Dependent Kinase 7 Promotes Th17/Th1 Cell Differentiation in Psoriasis by Modulating Glycolytic Metabolism. [Abstract]2021 Nov;141(11):2656-2667.e11. PMID: 34004188 -
Mol Cancer Ther
2025 Dec 4. PMID: 41340469 -
Mol Cancer Ther
Preclinical Efficacy and Molecular Mechanism of Targeting CDK7-Dependent Transcriptional Addiction in Ovarian Cancer. [Abstract]2017 Sep;16(9):1739-1750. PMID: 28572168
THZ1 Hydrochloride 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 Hydrochloride 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 Hydrochloride 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.
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JCI Insight
Anoikis resistance and metastasis of ovarian cancer can be overcome by CDK8/19 mediator kinase inhibition. [Abstract]2026 Jan 15;11(4):e192113. PMID: 41538289 -
Breast Cancer Res
Systematic screening identifies ABCG2 as critical factor underlying synergy of kinase inhibitors with transcriptional CDK inhibitors. [Abstract]2023 May 5;25(1):51. PMID: 37147730 -
Cells
Transcriptional CDK Inhibitors CYC065 and THZ1 Induce Apoptosis in Glioma Stem Cells Derived from Recurrent GBM. [Abstract]2021 May 12;10(5):1182. PMID: 34066147 -
Oncogenesis
SOX9 interacts with FOXC1 to activate MYC and regulate CDK7 inhibitor sensitivity in triple-negative breast cancer. [Abstract]2020 May 12;9(5):47. PMID: 32398735 -
Cells
CDK7 Inhibition is Effective in all the Subtypes of Breast Cancer: Determinants of Response and Synergy with EGFR Inhibition. [Abstract]2020 Mar 6;9(3):638. PMID: 32155786 -
Cells
Modulation of the Pol II CTD Phosphorylation Code by Rac1 and Cdc42 Small GTPases in Cultured Human Cancer Cells and Its Implication for Developing a Synthetic-Lethal Cancer Therapy. [Abstract]2020 Mar 4;9(3):621. PMID: 32143485 -
Cells
2019 Oct 6;8(10):1208. PMID: 31590445 -
Oncogenesis
2017 May 15;6(5):e336. PMID: 28504693
THZ1 Hydrochloride 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.
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Eur J Pharmacol
N76-1, a novel CDK7 inhibitor, exhibits potent anti-cancer effects in triple negative breast cancer. [Abstract]2023 Sep 15:955:175892. PMID: 37429520 -
Cell Oncol (Dordr)
2021 Aug;44(4):871-887. PMID: 33905040 -
mBio
Functional insight into cyclin-dependent kinase (CDK)7 via chemical inhibition of the priority fungal pathogen Cryptococcus neoformans. [Abstract]2025 Dec 10;16(12):e0289825. PMID: 41171060 -
PLoS Pathog
Epstein-Barr virus-transformed B-cells from a hypoxia model of the germinal center requires external unsaturated fatty acids. [Abstract]2025 Nov 11;21(11):e1013694. PMID: 41218077 -
Sci Rep
Selective but not pan-CDK inhibition abrogates 5-FU-driven tissue factor upregulation in colon cancer. [Abstract]2024 May 8;14(1):10582. PMID: 38719932 -
PLoS Pathog
A novel and ubiquitous miRNA-involved regulatory module ensures precise phosphorylation of RNA polymerase II and proper transcription. [Abstract]2024 Apr 19;20(4):e1012138. PMID: 38640110 -
Cancers (Basel)
BET and CDK Inhibition Reveal Differences in the Proliferation Control of Sympathetic Ganglion Neuroblasts and Adrenal Chromaffin Cells. [Abstract]2022 Jun 1;14(11):2755. PMID: 35681734 -
iScience
Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. [Abstract]2024 May 16;27(6):110011. PMID: 38868181 -
Front Mol Biosci
2021 Aug 19;8:697457. PMID: 34490348 -
Biochim Biophys Acta Mol Cell Res
CDK7 is a component of the integrated stress response regulating SNAT2 (SLC38A2)/System A adaptation in response to cellular amino acid deprivation. [Abstract]2019 Jun;1866(6):978-991. PMID: 30857869 -
Drug Dev Res
Disruption of the FOXM1 Regulatory Region Inhibits Tumor Progression in Ovarian Cancer by CRISPR-Cas9. [Abstract]2025 Feb;86(1):e70049. PMID: 39829431 -
FEBS J
Nuclear patterns of phosphatidylinositol 4,5- and 3,4-bisphosphate revealed by super-resolution microscopy differ between the consecutive stages of RNA polymerase II transcription. [Abstract]2024 Oct;291(19):4240-4264. PMID: 38734927 -
Front Oncol
Targeting Mutated p53 Dependency in Triple-Negative Breast Cancer Cells Through CDK7 Inhibition. [Abstract]2021 May 24;11:664848. PMID: 34109118 -
Front Oncol
CDK7 Inhibitor THZ1 Induces the Cell Apoptosis of B-Cell Acute Lymphocytic Leukemia by Perturbing Cellular Metabolism. [Abstract]2021 Apr 6:11:663360. PMID: 33889549 -
IUBMB Life
Cyclin-dependent kinase 7 is essential for spermatogenesis by regulating retinoic acid signaling pathways and the STAT3 molecular pathway. [Abstract]2021 Dec;73(12):1446-1459. PMID: 34717033 -
Biochem Biophys Res Commun
Super-enhancer-associated EEPD1 facilitates EMT-mediated metastasis by regulating the PI3K/AKT/mTOR pathway in gastric cancer. [Abstract]2023 Dec 31:689:149188. PMID: 37976838 -
J Mol Neurosci
Identification of Four Enhancer-Associated Genes as Risk Signature for Diffuse Glioma Patients. [Abstract]2022 Feb;72(2):410-419. PMID: 34462884 -
Onco Targets Ther
CDK7 inhibitor suppresses tumor progression through blocking the cell cycle at the G2/M phase and inhibiting transcriptional activity in cervical cancer. [Abstract]2019 Mar 22:12:2137-2147. PMID: 30962695
THZ1 Hydrochloride 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.
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Res Sq
Epstein-Barr Virus-Driven B-Cell Transformation under Germinal Center Hypoxia Requires External Unsaturated Fatty Acids. [Abstract]2025 Apr 24:rs.3.rs-6506954. PMID: 40313738 -
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Heliyon
Co-overexpression of BRD4 and CDK7 promotes cell proliferation and predicts poor prognosis in HCC. [Abstract]2024 Jan 9;10(2):e24389. PMID: 38293462 -
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Oncotarget
Essential role of endogenous prolactin and CDK7 in estrogen-induced upregulation of the prolactin receptor in breast cancer cells. [Abstract]2017 Apr 18;8(16):27353-27363. PMID: 28423697
THZ1 Hydrochloride 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.
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THZ1 Hydrochloride 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.
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Harvard Medical School LINCS LIBRARY
Solvant et solubilité
In Vitro:
DMSO : 116.67 mg/mL (193.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (3.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.17 mg/mL (3.60 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.17 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (286 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20. [Content Brief]
[2]. Jiang YY, et al. Targeting super-enhancer-associated oncogenes in oesophageal squamous cell carcinoma. Gut. 2016 May 10. pii: gutjnl-2016-311818. [Content Brief]
[3]. Christensen CL, et al. Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. Cancer Cell. 2014 Dec 8;26(6):909-22. [Content Brief]
[4]. Chipumuro, et al. CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 2014 Nov 20;159(5):1126-39. ? [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.6597 mL | 8.2986 mL | 16.5972 mL | 41.4931 mL |
| 5 mM | 0.3319 mL | 1.6597 mL | 3.3194 mL | 8.2986 mL | |
| 10 mM | 0.1660 mL | 0.8299 mL | 1.6597 mL | 4.1493 mL | |
| 15 mM | 0.1106 mL | 0.5532 mL | 1.1065 mL | 2.7662 mL | |
| 20 mM | 0.0830 mL | 0.4149 mL | 0.8299 mL | 2.0747 mL | |
| 25 mM | 0.0664 mL | 0.3319 mL | 0.6639 mL | 1.6597 mL | |
| 30 mM | 0.0553 mL | 0.2766 mL | 0.5532 mL | 1.3831 mL | |
| 40 mM | 0.0415 mL | 0.2075 mL | 0.4149 mL | 1.0373 mL | |
| 50 mM | 0.0332 mL | 0.1660 mL | 0.3319 mL | 0.8299 mL | |
| 60 mM | 0.0277 mL | 0.1383 mL | 0.2766 mL | 0.6916 mL | |
| 80 mM | 0.0207 mL | 0.1037 mL | 0.2075 mL | 0.5187 mL | |
| 100 mM | 0.0166 mL | 0.0830 mL | 0.1660 mL | 0.4149 mL |
THZ1 Hydrochloride Related Classifications
HY-80013A Related Classifications
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