CDK13
CDK13 is a transcription-associated cyclin-dependent kinase that forms a complex with cyclin K and regulates RNA polymerase II (RNAPII) activity through phosphorylation of the carboxy-terminal domain (CTD), thereby coupling transcription elongation with co-transcriptional RNA processing events[1][2]. Mechanistically, CDK13 cooperates with the closely related kinase CDK12 to control RNAPII elongation rate, processivity, transcription termination site selection, and alternative polyadenylation, establishing a central role in global gene-expression regulation[3]. CDK13 also contributes to mRNA splicing control, and dual CDK12/CDK13 inhibition disrupts splicing of promoter-proximal introns containing weak splice-site features, linking CDK13 activity to RNA maturation pathways[4]. In disease-relevant models, deregulation of CDK12/CDK13-dependent transcription affects genome stability programs and has been associated with tumor biology, replication stress responses, and altered expression of genes involved in RNA processing and DNA damage repair[2][3][5]. Compared with CDK12, which preferentially supports transcription of DNA damage response genes, CDK13 exerts stronger effects on splicing and RNA-processing networks, highlighting partially overlapping but nonidentical biological functions between the two paralogous kinases[2][6]. For experimental applications, covalent CDK12/CDK13 inhibitors such as THZ531 have been widely used to interrogate transcription elongation, CTD phosphorylation, alternative polyadenylation, and RNA-processing mechanisms in cancer and transcription-focused research models[3][4].
References:
- [1]. Blazek D, et al. The Cyclin K/Cdk12 complex maintains genomic stability via regulation of expression of DNA damage response genes. Genes Dev. 2011 Oct 15;25(20):2158-72. [Content Brief]
- [2]. Pitolli C, et al. Physiological and pathological roles of the transcriptional kinases CDK12 and CDK13 in the central nervous system. Cell Death Differ. 2025 Mar;32(3):371-381. [Content Brief]
- [3]. 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]
- [4]. Panzeri V, et al. CDK12/13 promote splicing of proximal introns by enhancing the interaction between RNA polymerase II and the splicing factor SF3B1. Nucleic Acids Res. 2023 Jun 23;51(11):5512-5526. [Content Brief]
- [5]. Krajewska M, et al. CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation. Nat Commun. 2019 Apr 15;10(1):1757. [Content Brief]
- [6]. Dudkiewicz-Garbicz J, et al. CDK12 and CDK13 in oncology: from RNA regulation to therapeutic targeting. Cell Oncol (Dordr). 2026 Jan 5;49(1):13. [Content Brief]
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CDK13 Related Products (25)
Related Products (25)
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YJ1206
0 ImagesCat. No.: HY-168555CAS No.: 3053716-98-3YJ1206 is an orally active selective CDK12/CDK13 PROTAC degrader. YJ1206 induces DNA damage and genomic instability, activates the AKT pathway, and triggers apoptosis. YJ1206 reduces tumor cell viability, inhibits tumor growth, and attenuates tumor cell dissemination. YJ1206 is applicable to research related to prostate cancer and high-grade serous tubo-ovarian cancer.
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DN1679
0 ImagesCat. No.: HY-181035DN1679 is a potent, selective and orally active CRBN-dependent CDK12/13 PROTAC dual degrader. DN1679 shows DC50 of 8.8/9.8 nM (MDA-MB-231), 5.1/6.4 nM (MDA-MB-157) and 17.2/15.8 nM (MDA-MB-468) for CDK12/13. DN1679 can downregulate DNA damage response gene mRNA levels, such as ATM, ATR, BRCA1 and RAD51. DN1679 demonstrates a potent synergistic anti-tumor effect companied with Olaparib (HY-10162). DN1679 can be used for research of triple-negative breast cance.
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CDK12-IN-9
0 ImagesCat. No.: HY-181645CAS No.: 3024723-74-5
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MFH290
0 ImagesMFH290 is an orally active, selective covalent CDK12/CDK13 inhibitor, with an IC50 of 25 nM against human CDK12 and 49 nM against human CDK13. MFH290 reduces the phosphorylation level of CTD-RNAPII-Ser2, downregulates genes related to DNA damage response (DDR), and inhibits transcription factors regulated by super-enhancers. MFH290 can be used in research related to various cancers including leukemia.
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PROTAC CDK12/13 Degrader-1 TFA
0 ImagesCat. No.: HY-151110APurity: 99.12%
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ZLC491
0 ImagesZLC491 is an orally active PROTAC degrader that selectively targets CDK12/CDK13 and exhibits certain oral bioavailability. ZLC491 induces cereblon- and proteasome-dependent selective degradation of CDK12 and CDK13. ZLC491 inhibits the transcription and expression of long genes, and mainly acts on a subset of DNA damage response genes. ZLC491 inhibits the proliferation of various triple-negative breast cancer cells. ZLC491 can be used in research related to triple-negative breast cancer.
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YJ9069
0 ImagesCat. No.: HY-168556YJ9069 is a CDK12/CDK13 PROTAC degrader. YJ9069 induces proteasome-dependent degradation of CDK12 and CDK13, and inhibits serine 2 phosphorylation of RNA polymerase II (RNA polymerase II). YJ9069 triggers gene length-dependent transcription elongation defects, reduces the expression of DNA damage response genes, and induces DNA damage, cell cycle arrest and apoptosis. YJ9069 inhibits tumor growth in prostate cancer models. YJ9069 can be used for the research of prostate cancer, Ewing sarcoma and breast cancer.
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CDK12/13-IN-3
0 ImagesCDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6%.
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CDK6/PIM1-IN-1
0 ImagesCat. No.: HY-142696CAS No.: 2677026-14-9CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity.
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CDK7-IN-28
0 ImagesCat. No.: HY-158170CAS No.: 3034082-58-8CDK7-IN-28 (CDK7-1276) is a potent CDK7 inhibitor(IC50＜5 nM). CDK7-IN-28 can inhibit proliferation of MDA-MB-468 cell line by blocking cell cycle and inhibiting DNA replication.
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CDK12/13-IN-2
0 ImagesCat. No.: HY-173042CAS No.: 3076450-41-1
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SR-5037
0 ImagesSR-5037 is an orally active CDK12 (IC50 = 31 nM)/CDK13 inhibitor and CycK (DC50 = 30 nM; Dmax > 98%) molecular glue degrader. SR-5037 inhibits the enzymatic activity of CDK12/CycK and CDK13/CycK complexes. SR-5037 promotes the recruitment of DDB1 to the CDK12/CycK complex, thereby triggering proteasome-mediated CycK degradation. SR-5037 degrades active CycK in mouse models of triple-negative breast cancer. SR-5037 can be used in the research of cancers such as triple-negative breast cancer.
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