CDK9
CDK9 (cyclin-dependent kinase 9) is a transcription-associated serine/threonine kinase that functions as the catalytic subunit of positive transcription elongation factor b (P-TEFb) and regulates productive RNA polymerase II (RNAPII) elongation through phosphorylation of the RNAPII C-terminal domain and elongation factors.[1][2] Mechanistically, CDK9-cyclin T complexes promote release of promoter-proximally paused RNAPII into gene bodies, thereby controlling transcriptional programs required for cellular responses to developmental and environmental signals.[1][2] Beyond transcriptional elongation, CDK9 contributes to transcription initiation, termination, and maintenance of appropriate transcriptional output, highlighting its central role in gene expression regulation.[1] Dysregulated CDK9 activity has been linked to multiple pathological conditions, particularly cancer, where aberrant transcriptional dependencies create vulnerability to pharmacological CDK9 inhibition.[1][3] In cancer models, activation of P-TEFb-dependent transcription supports oncogenic pathways including MYC, NF-κB, and stress-response signaling, and selective suppression of CDK9 can induce apoptotic programs and impair tumor cell proliferation.[4] Compared with related transcriptional cyclin-dependent kinases such as CDK12 and CDK13, which primarily regulate distinct transcriptional and RNA-processing programs through cyclin K-containing complexes, CDK9 acts as the principal P-TEFb kinase controlling promoter-proximal pause release and rapid transcriptional activation.[1][5] For experimental applications, small-molecule CDK9 inhibitors including flavopiridol have been widely used to suppress RNAPII-dependent transcription, investigate transcriptional addiction, and evaluate therapeutic vulnerabilities associated with transcriptional dysregulation.[1][6]
References:
- [1]. Egloff S. CDK9 keeps RNA polymerase II on track. Cell Mol Life Sci. 2021 Jul;78(14):5543-5567. [Content Brief]
- [2]. Anshabo AT, et al. CDK9: A Comprehensive Review of Its Biology, and Its Role as a Potential Target for Anti-Cancer Agents. Front Oncol. 2021 May 10;11:678559. [Content Brief]
- [3]. Constantin TA, et al. Transcription associated cyclin-dependent kinases as therapeutic targets for prostate cancer. Oncogene. 2022 Jun;41(24):3303-3315. [Content Brief]
- [4]. Yuan B, et al. Engineering of cytosine base editors with DNA damage minimization and editing scope diversification. Nucleic Acids Res. 2023 Nov 10;51(20):e105. [Content Brief]
- [5]. Fan Z, et al. CDK13 cooperates with CDK12 to control global RNA polymerase II processivity. Sci Adv. 2020 Apr 29;6(18):eaaz5041. [Content Brief]
- [6]. Phiel CJ, et al. Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. J Biol Chem. 2001 Sep 28;276(39):36734-41. [Content Brief]
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CDK9 Related Products (206)
Related Products (206)
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Antibodies (1)
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CDK9/HDAC1/HDAC3-IN-1
0 ImagesCat. No.: HY-172891CAS No.: 2197029-81-3CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC50 s of 0.17 μM, 1.73 μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer.
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CDK9-IN-50
0 ImagesCat. No.: HY-183710CAS No.: 3114520-65-6CDK9-IN-50 is a selective and orally active CDK9 inhibitor with an IC50 of 2.2 nM. CDK9-IN-50 targets a distinct CDK9-specific subpocket to disrupt RNA polymerase II Ser2 phosphorylation and downregulate short-lived oncoproteins, including AR-V7 and Myc. CDK9-IN-50 exhibits antiproliferative activity against cancer cells, induces apoptosis and induces tumor growth inhibition in CRPC orthotopic mice models. CDK9-IN-50 can be used for the research of cancer, such as prostate cancer.
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CDK9-IN-19
0 ImagesCat. No.: HY-150562CAS No.: 2479306-60-8CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML).
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CDK9-IN-22
0 ImagesCat. No.: HY-151984CAS No.: 2872677-61-5
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CDK9-IN-48
0 ImagesCat. No.: HY-185339CAS No.: 2987897-20-9CDK9-IN-48 is a CDK9 inhibitor with an IC50 of 1.37 nM. CDK9-IN-48 inhibits the proliferation of various cancer cells. CDK9-IN-48 can be used in the research of cancers such as acute myeloid leukemia and prostate cancer.
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BLINK11
0 ImagesCat. No.: HY-173347BLINK11 is a BBB-penetrant CDK5 inhibitor. BLINK11 lowers CDK5 activity for both complexes CDK5/p35 (IC50 = 17.09 nM) and CDK5/p25 (IC50 = 14.69 nM). BLINK11 offers anti-diabetic and neuroprotective benefits. BLINK11 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.
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IIIM-290
0 ImagesCat. No.: HY-111356CAS No.: 2213468-64-3IIIM-290 is a potent and oral CDK inhibitor with IC50s of 90 and 94 nM for CDK2/A and CDK9/T1.
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FLT3/CDKs ligand-1
0 ImagesCat. No.: HY-161709CAS No.: 2452019-67-7FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708).
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CDK9-IN-46
0 ImagesCat. No.: HY-181569CAS No.: 2620706-60-5
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CDK9-IN-40
0 ImagesCat. No.: HY-176736CDK9-IN-40 is a potent and orally active CDK9 inhibitor with an IC50 of 5.5 nM. CDK9-IN-40 shows high selectivity for CDK9 versus CDK1, CDK2, CDK4, and CDK6, respectively. CDK9-IN-40 can arrest cell cycle, induce cell apoptosis and inhibit tumor growth. CDK9-IN-40 exhibits strong anti-cancer activity.
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CDK9-IN-52
0 ImagesCat. No.: HY-183699CDK9-IN-52 is a CDK9 inhibitor. CDK9-IN-52 exhibits antiproliferative activity against cancer cells. CDK9-IN-52 can be used in studies related to lung cancer, cervical cancer, and breast cancer.
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PROTAC CDK9 degrader-13
0 ImagesCat. No.: HY-184693PROTAC CDK9 degrader-13 is a selective CDK9 degrader acting via the ubiquitin-proteasome system. PROTAC CDK9 degrader-13 induces apoptosis in acute myeloid leukemia cells. PROTAC CDK9 degrader-13 suppresses tumor growth in vivo and has a defined safety profile. PROTAC CDK9 degrader-13 can be used for the research of acute myeloid leukemia.
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PROTAC CDK9 degrader-14
0 ImagesCat. No.: HY-133617CAS No.: 2411019-98-0PROTAC CDK9 degrader-14 is a CDK9 PROTAC degrader that recruits CRBN. PROTAC CDK9 degrader-14 efficiently degrades CDK9 and inhibits cell proliferation in solid tumors and hematological malignancies. PROTAC CDK9 degrader-14 can be used in research related to solid tumors, hematological malignancies and triple-negative breast cancer.
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CDK9-IN-53
0 ImagesCat. No.: HY-13828CAS No.: 1421340-50-2CDK9-IN-53 is a potent and selective CDK9 inhibitor with a Ki of 7 nM and an IC50 of 14 nM against CDK9/Cyclin T1. CDK9-IN-53 achieves highly selective inhibition by competitively binding to the ATP pocket of CDK9, thereby blocking RNAPII transcription and downregulating the anti-apoptotic protein Mcl-1, ultimately triggering Caspase-dependent apoptosis in cancer cells. CDK9-IN-53 can be used for research on chronic lymphocytic leukemia.
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CDK7-IN-20
0 ImagesCat. No.: HY-151878CAS No.: 3034210-97-1
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CDK9 ligand 4
0 ImagesCat. No.: HY-181275CAS No.: 2609749-29-1CDK9 ligand 4 is a CDK9 ligand. As a ligand for target protein for PROTAC (Ligands for Target Protein for PROTAC), CDK9 ligand 4 serves for the development and design of PROTAC CDK9 degraders, such as PROTAC CDK9 degrader-12 (HY-181231). CDK9 ligand 4 is applicable to the research of HIV-1 infection.
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CDK9 autophagic degrader 1
0 ImagesCat. No.: HY-168896CAS No.: 3066836-42-5CDK9 autophagic degrader 1 (Compound 28) is a ATTEC degrader that can be used to degrade CDK9 and also affects the levels of the associated Cyclin T1. CDK9 autophagic degrader 1 shows over 80% CDK9 inhibition rate at 100 nM. ( Pink: LC3B ligand (HY-168897); Black: linker (HY-W017758); Blue: target protein ligand (HY-10008); linker + target protein ligand (HY-168898))
