1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK7 Isoform

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:

Cat. No. Product Name Effect Purity
  • HY-16297A
    Abemaciclib
    Inhibitor 99.97%
    Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
  • HY-80013
    THZ1
    Inhibitor 99.84%
    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.
  • HY-16297
    Abemaciclib methanesulfonate
    Inhibitor 99.95%
    Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective and BBB-permeable CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.
  • HY-10008
    SNS-032
    Inhibitor 99.91%
    SNS-032 (BMS-387032) is a potent and selective inhibitor of CDK2, CDK7, and CDK9 with IC50s of 38 nM, 62 nM and 4 nM, respectively. SNS-032 has antitumor effect.
  • HY-103618
    THZ531
    Inhibitor 99.86%
    THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.
  • HY-153278A
    Q901 TFA
    Inhibitor
    Q901 (CDK7-IN-21) TFA is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 TFA disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 TFA can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 TFA can be used for the research of cancer, such as colon cancer and lung cancer.
  • HY-172194A
    (S)-JNJ-3738
    Inhibitor
    (S)-JNJ-3738 is a CDK7 inhibitor. (S)-JNJ-3738 regulates kinase activity and exerts weak inhibitory effects on the activity of mutant CDK7. (S)-JNJ-3738 is applicable for cancer research.
  • HY-181528
    JAK1/CDK7-IN-1
    Inhibitor
    JAK1/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.
  • HY-138293
    SY-5609
    Inhibitor 99.93%
    SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (Ki=2600 nM), CDK9 (Ki=960 nM), CDK12 (Ki=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity.
  • HY-103712A
    Samuraciclib hydrochloride
    Inhibitor 99.98%
    Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects.
  • HY-103248
    Toyocamycin
    Inhibitor 99.27%
    Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM.
  • HY-101257
    YKL-5-124
    Inhibitor 99.53%
    YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-X0009
    Tambiciclib
    Inhibitor 99.21%
    Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib can be used for AML research.
  • HY-50940
    AT7519
    Inhibitor 99.69%
    AT7519 (AT7519M) as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
  • HY-10012
    AZD-5438
    Inhibitor 99.91%
    AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 .
  • HY-123954
    BTX-A51
    Inhibitor 98.58%
    BTX-A51 (Casein Kinase inhibitor A51) is a potent and orally active casein kinase 1α (CK1α) inhibitor. BTX-A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
  • HY-18340
    (R)​-​CR8
    Inhibitor 99.52%
    (R)-CR8, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.
  • HY-128587
    Mevociclib
    Inhibitor 99.73%
    Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
  • HY-137478
    KB-0742
    Inhibitor 99.63%
    KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity.
  • HY-137478A
    KB-0742 dihydrochloride
    Inhibitor 98.77%
    KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity