Human Recombinant CDK12 protein, GST Tag (V2LY-0526-LY3022)

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Basic Information

Expressed Host
Baculovirus-Insect Cells
Protein Species
Human
Tag
GST Tag
Protein Construction
This product is Human Recombinant CDK12 protein, GST Tag consist of Amino Acid: 658-end and predicts a molecular mass of 135 kDa.
Molecule Mass
135 kDa
Sequence
Amino Acid: 658-end
Species
Human

Formulations & Storage [For reference only, actual COA shall prevail!]

Purity
Batch dependent.
Endotoxin
Please contact us for more information.
Format
Liquid
Buffer
Please contact us for more information.
Preservative
None
Storage
Store product at -70°C. For optimal storage, aliquot target into smaller quantities after centrifugation and store at recommended temperature. For most favorable performance, avoid repeated handling and multiple freeze/thaw cycles.
More Infomation

Target

Full Name
cyclin-dependent kinase 12
Function
Cyclin-dependent kinase that phosphorylates the C-terminal domain (CTD) of the large subunit of RNA polymerase II (POLR2A), thereby acting as a key regulator of transcription elongation. Regulates the expression of genes involved in DNA repair and is required for the maintenance of genomic stability. Preferentially phosphorylates 'Ser-5' in CTD repeats that are already phosphorylated at 'Ser-7', but can also phosphorylate 'Ser-2'. Required for RNA splicing, possibly by phosphorylating SRSF1/SF2. Involved in regulation of MAP kinase activity, possibly leading to affect the response to estrogen inhibitors.
Biological Process
mRNA processing Source: UniProtKB-KW
Negative regulation of stem cell differentiation Source: Ensembl
Phosphorylation of RNA polymerase II C-terminal domain Source: UniProtKB
Positive regulation of transcription elongation from RNA polymerase II promoter Source: GO_Central
Protein autophosphorylation Source: HGNC-UCL
Protein phosphorylation Source: GO_Central
Regulation of MAP kinase activity Source: UniProtKB
Regulation of RNA splicing Source: Ensembl
RNA splicing Source: UniProtKB
Transcription elongation from RNA polymerase II promoter Source: GO_Central
Cellular Location
Nucleus; Nucleus speckle. Colocalized with nuclear speckles throughout interphase.
Involvement in disease
Chromosomal aberrations involving CDK12 may be a cause gastric cancer. Deletions within 17q12 region producing fusion transcripts with ERBB2, leading to CDK12-ERBB2 fusion leading to trunctated CDK12 protein not in-frame with ERBB2.
PTM
Phosphorylation at Thr-893 increases kinase activity.

Liu, H., Liu, K., & Dong, Z. (2021). Targeting CDK12 for cancer therapy: function, mechanism, and drug discovery. Cancer research, 81(1), 18-26.

Rescigno, P., Gurel, B., Pereira, R., Crespo, M., Rekowski, J., Rediti, M., ... & de Bono, J. S. (2021). Characterizing CDK12-mutated prostate cancers. Clinical Cancer Research, 27(2), 566-574.

Reimers, M. A., Yip, S. M., Zhang, L., Cieslik, M., Dhawan, M., Montgomery, B., ... & Chou, J. (2020). Clinical outcomes in cyclin-dependent kinase 12 mutant advanced prostate cancer. European urology, 77(3), 333-341.

Liu, Y., Hao, M., Leggett, A. L., Gao, Y., Ficarro, S. B., Che, J., ... & Gray, N. S. (2020). Discovery of MFH290: a potent and highly selective covalent inhibitor for cyclin-dependent kinase 12/13. Journal of Medicinal Chemistry, 63(13), 6708-6726.

Thanindratarn, P., Dean, D. C., Feng, W., Wei, R., Nelson, S. D., Hornicek, F. J., & Duan, Z. (2020). Cyclin-dependent kinase 12 (CDK12) in chordoma: prognostic and therapeutic value. European Spine Journal, 29(12), 3214-3228.

Liang, S., Hu, L., Wu, Z., Chen, Z., Liu, S., Xu, X., & Qian, A. (2020). CDK12: A potent target and biomarker for human cancer therapy. Cells, 9(6), 1483.

Emadi, F., Teo, T., Rahaman, M. H., & Wang, S. (2020). CDK12: a potential therapeutic target in cancer. Drug Discovery Today.

Antonarakis, E. S. (2018). Cyclin-dependent kinase 12, immunity, and prostate cancer. New England Journal of Medicine, 379(11), 1087-1089.

Lui, G. Y., Grandori, C., & Kemp, C. J. (2018). CDK12: an emerging therapeutic target for cancer. Journal of clinical pathology, 71(11), 957-962.

Johannes, J. W., Denz, C. R., Su, N., Wu, A., Impastato, A. C., Mlynarski, S., ... & Guichard, S. (2018). Structure‐Based Design of Selective Noncovalent CDK12 Inhibitors. ChemMedChem, 13(3), 231-235.

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For research use only. Not intended for any clinical use.

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