CDK7
CDK7 (cyclin-dependent kinase 7) functions as a dual-regulatory kinase that coordinates cell-cycle progression and RNA polymerase II-dependent transcription through its activity within the CDK-activating kinase (CAK) complex and the general transcription factor TFIIH complex[1][2][3]. CDK7 phosphorylates and activates multiple cell-cycle CDKs, including CDK1, CDK2, CDK4, and CDK6, thereby linking transcriptional control to cell-cycle regulation[1][4]. Mechanistically, TFIIH-associated CDK7 phosphorylates the C-terminal domain (CTD) of RNA polymerase II and promotes transcription initiation, promoter clearance, and productive promoter escape[2][5][6]. CDK7 further regulates transcriptional programs through phosphorylation-dependent control of transcription-associated kinases and RNA processing factors, supporting coordinated gene expression in proliferating cells[2]. In disease models, aberrant CDK7 activity is associated with tumor cell proliferation and transcriptional dependency, making CDK7 a relevant target for cancer research and therapeutic intervention[1][7]. Compared with related CDK family members that primarily regulate discrete cell-cycle transitions, CDK7 uniquely combines CAK activity with direct transcriptional regulation through TFIIH, establishing a distinct functional position within the CDK network[4][6]. For experimental applications, selective CDK7 inhibitors have enabled mechanistic dissection of transcription initiation, RNA polymerase II dynamics, and transcriptional kinase signaling, supporting their broad use in functional genomics and oncology research[2][5].
References:
- [1]. Reiss HD, et al. Nifedipine-sensitive calcium channels are involved in polar growth of lily pollen tubes. J Cell Sci. 1985;76(1):247-254.
- [2]. Rimel JK, et al. Selective inhibition of CDK7 reveals high-confidence targets and new models for TFIIH function in transcription. Genes Dev. 2020 Nov 1;34(21-22):1452-1473. [Content Brief]
- [3]. Lee MJ, et al. Time to HIV rebound after infusion of long-acting broadly neutralising antibodies 3BNC117-LS and 10-1074-LS and analytical treatment interruption (the RIO trial): a double-blind, randomised, placebo-controlled trial. Lancet HIV. 2026 May 27:S2352-3018(26)00059-7. [Content Brief]
- [4]. Wood DJ, et al. Structural insights into the functional diversity of the CDK-cyclin family. Open Biol. 2018 Sep;8(9):180112. [Content Brief]
- [5]. Žumer K, et al. FACT maintains chromatin architecture and thereby stimulates RNA polymerase II pausing during transcription in vivo. Mol Cell. 2024 Jun 6;84(11):2053-2069.e9. [Content Brief]
- [6]. Fisher RP. Cdk7: a kinase at the core of transcription and in the crosshairs of cancer drug discovery. Transcription. 2019 Apr;10(2):47-56. doi: 10.1080/21541264.2018.1553483. Epub 2018 Dec 6. PMID: 30488763; PMCID: PMC6602562. et al. Cdk7: a kinase at the core of transcription and in the crosshairs of cancer drug discovery. Transcription. 2019 Apr;10(2):47-56. [Content Brief]
- [7]. Jones T, et al. TFIIH kinase CDK7 drives cell proliferation through a common core transcription factor network. Sci Adv. 2025 Feb 28;11(9):eadr9660. [Content Brief]
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CDK7 Related Products (118)
Related Products (118)
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Recombinant Proteins (4)
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Antibodies (3)
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CDK7-IN-16
0 ImagesCat. No.: HY-147601CAS No.: 2765676-32-0CDK7-IN-16 (compound 9) is a potent CDK 7 inhibitor with an IC50 range of 1 ~ 10 nM. CDK7-IN-16 can be used for researching anticancer, especially the cancer with transcriptional dysregulation.
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CDK7-IN-10
0 ImagesCat. No.: HY-145424CAS No.: 2588110-62-5
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HDAC1/CDK7-IN-1
0 ImagesCat. No.: HY-156444CAS No.: 2987905-95-1HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells.
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CDKI-83
0 ImagesCat. No.: HY-123034CAS No.: 1189558-88-0CDKI-83 is a potent CDK9 and CDK1 inhibitor with Ki values of 21 nM and 72 nM for CDK9/T1 and CDK1/B, respectively. CDKI-83 demonstrates effective anti-proliferative activity in human tumour cell lines with a GI50<1 μM. CDKI-83 effectively induces apoptosis in A2780 human ovarian cancer cells. CDKI-83 reduces phosphorylation at Ser-2 of RNA polymerase II (RNAPII) by inhibiting cellular CDK9 activity, and down-regulates Mcl-1 and Bcl-2. CDKI-83 has the potential for anti-cancer research.
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CDK7-IN-32
0 ImagesCat. No.: HY-170425CAS No.: 2055741-42-7CDK7-IN-32 (compound10) is a CDK7 inhibitor.
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PI3Kα/CDK7-IN-1
0 ImagesCat. No.: HY-187454PI3Kα/CDK7-IN-1 is a dual-target hybrid inhibitor of PI3Kα and CDK7, with IC50 values of 87.9 nM and 638 nM, respectively. PI3Kα/CDK7-IN-1 acts as a cytotoxic agent and cell death inducer that triggers apoptotic death in cancer cells. PI3Kα/CDK7-IN-1 can be used in cancer research such as colorectal cancer.
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JAK1/CDK7-IN-1
0 ImagesCat. No.: HY-181528JAK1/CDK7-IN-1 is a JAK1/CDK7 inhibitor. JAK1/CDK7-IN-1 forms a stable and tightly bound complex with JAK1. JAK1/CDK7-IN-1 disrupts the cell cycle, induces G2/M phase arrest, and increases the proportion of pre-G1 phase cells. JAK1/CDK7-IN-1 induces cellular apoptosis (apoptosis) and necrosis. JAK1/CDK7-IN-1 is applicable to research related to breast cancer and prostate cancer.
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CDK7 ligand 3
0 ImagesCat. No.: HY-183071CAS No.: 3040999-61-6CDK7 ligand 3 is a target protein ligand for CXJ2080 (HY-183070), which be used for the research of acute leukemia.
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CXJ2080
0 ImagesCat. No.: HY-183070CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC50 of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia.
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CDK9-IN-33
0 ImagesCat. No.: HY-162619CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC50 values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity.
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CDK/HDAC-IN-2
0 ImagesCat. No.: HY-146276CAS No.: 2580938-58-3CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy.
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CDK7-IN-20
0 ImagesCat. No.: HY-151878CAS No.: 3034210-97-1
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CDK2-IN-47
0 ImagesCat. No.: HY-178112CDK2-IN-47 is a potent CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer.
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ZJC-11
0 ImagesCat. No.: HY-189062ZJC-11 is a CDK7 inhibitor with an IC50 of 5.4 nM. ZJC-11 binds covalently to CDK7, inhibits CDK7-dependent phosphorylation of RNAPII at Ser2, Ser5 and Ser7 sites, and suppresses transcriptional processes. ZJC-11 acts as a cell cycle inhibitor, inhibits the G2/M checkpoint pathway, and induces G2/M phase arrest. ZJC-11 induces DNA damage-driven cellular senescence and cell death. ZJC-11 exhibits antiproliferative activity against triple-negative breast cancer both in vitro and in vivo. ZJC-11 can be used for research related to triple-negative breast cancer
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CDK8-IN-20
0 ImagesCat. No.: HY-180124CDK8-IN-20 (Compound 67j) is a selective, potent and orally active type I CDK8 inhibitor with an IC50 of 70.5 nM. CDK8-IN-20 shows IC50 values of 147.8, 726.9 and 217.4 nM for homologous kinase CDK19, CDK7 and CDK9. CDK8-IN-20 can inhibit the Wnt/β-catenin pathway and downregulate the expression of β-catenin, Cyclin D1, and c-Myc. CDK8-IN-20 can induce ROS production and cause G2/M and S phase arrest. CDK8-IN-20can be used for the research of cancer, such as colon cancer.
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KB-0742 hydrochloride
0 ImagesCat. No.: HY-137478B
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SZ-015268
0 ImagesCat. No.: HY-145389CAS No.: 2654003-68-4SZ-015268 is a CDK7 inhibitor with an IC50 of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC50s of 33, 80.56, 12.53, and 61.55 nM, respectively.
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CDK7-IN-8
0 ImagesCat. No.: HY-143586CAS No.: 2654003-64-0
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SY-5102
0 ImagesCat. No.: HY-180355CAS No.: 2365230-48-2SY-5102 is a potent, selective, and orally active cyclin-dependent kinase (CDK7) inhibitor with a Kd value of 0.03 nM. SY-5102 occupies the ATP-binding pocket of CDK7 via non-covalent binding to inhibit CDK7 activity, and downregulates its phosphorylation of cyclin CDK and RNA polymerase II. SY-5102 inhibits cancer cell proliferation, and induces tumor growth inhibition and regression. SY-5102 can be used in research related to triple-negative breast cancer.
