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dCeMM3 (Compound 3) is a glue degrader. dCeMM3 induces ubiquitination and degradation of cyclinK by prompting an interaction of CDK12-cyclinK with a CRL4B ligase complex .
dCeMM4 (Compound 5) is a glue degrader. dCeMM4 induces ubiquitination and degradation of cyclinK by prompting an interaction of CDK12-cyclinK with a CRL4B ligase complex .
PP-C8 is a potent and selective PROTAC CDK12-CyclinK degrader. PP-C8 induces CDK12-CyclinK degradation with DC50s of 416 and 412 nM for CDK12 and CyclinK, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC) .
dCeMM2 (Compound 2) is a glue degrader. dCeMM2 induces ubiquitination and degradation of cyclinK by prompting an interaction of CDK12-cyclinK with a CRL4B ligase complex .
NCT02 is a cyclinK degrader. NCT02 induces ubiquitination of cyclinK (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. NCT02 has the potential for the research of metastatic colorectal cancer (CRC) .
HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclinK degradation. HQ461-mediated degradation of cyclinK impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death .
SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclinK, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer .
LL-K12-18 is a two-site molecular glue that enhances the protein-protein interaction of the CDK12-DDB1 complex, stabilizing the CDK12-DDB1 complex and promoting the degradation of cyclinK (EC50=0.37 nM). LL-K12-18 exhibits strong gene transcription inhibition and anti-proliferation effects in tumor cells. LL-K12-18 can be used in cancer research .
CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclinK and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II .
BSJ-5-63 is a potent CDK12, CDK7, CDK9 degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, CyclinK. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer .
H1k, a Eudistomin Y derivative, is a lysosome-targeted antiproliferation agent. H1k increases the autophagy signal and downregulate the expression of cyclin-dependent kinase (CDK1) and cyclin B1. H1k can be used in research of cancer .
K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively .
SLM6 is a sangivamycin-like molecule. SLM6 is a CDK9 inhibitor. SLM6 inhibits CDK9/cyclinK and CDK9/cyclin T1 kinase activity with IC50s of 280 nM and 133 nM, respectively. SLM6 also inhibits CDK1/cyclin B and CDK2/
cyclin A with IC50s of less than 300 nM. SLM6 induces apoptosis in multiple myeloma (MM) cells .
LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs .
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
LL-K8-22 is a potent, selective and durable CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research .
(R)-CR8 (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 cyclinK .
(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride 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 trihydrochloride induces apoptosis and has neuroprotective effect . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclinK .
The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNK Heterodimer Protein, Human (Sf9, GST, FLAG) is a recombinant protein dimer complex containing human-derived CDK12-CCNK Heterodimer protein, expressed by Sf9 insect cells , with N-Flag, N-GST labeled tag.
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNK Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK9-CCNK Heterodimer protein, expressed by Sf9 insect cells , with tag free.
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNK Heterodimer Protein, Human (Sf9, GST, FLAG) is a recombinant protein dimer complex containing human-derived CDK9-CCNK Heterodimer protein, expressed by Sf9 insect cells , with N-Flag, N-GST labeled tag.
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNT1 Protein, Human (sf9, GST, His) is the recombinant human-derived CDK9-CCNT1, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. ,
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNT2 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK9-CCNT2, expressed by Sf9 insect cells , with N-His, N-GST, N-Flag labeled tag. ,
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNT1 Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK9-CCNT1 Heterodimer protein, expressed by Sf9 insect cells , with tag free.
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8-CCNK Protein, Human (sf9, GST) is the recombinant human-derived CDK8-CCNK, expressed by Sf9 insect cells , with N-GST labeled tag. ,
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8 Protein, Human ( Unactive, sf9, GST) is the recombinant human-derived CDK8, expressed by Sf9 insect cells , with GST labeled tag. The total length of CDK8 Protein, Human ( Unactive, sf9, GST) is 464 a.a.,
The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNK Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK12-CCNK Heterodimer protein, expressed by Sf9 insect cells , with tag free.
The CDK9 protein plays a central role in transcriptional regulation, promoting the transition from ineffective to efficient elongation by phosphorylating POLR2A, SUPT5H, and RDBP. As part of the CDK9/cyclin-T complex, it participates in phosphorylation events affecting EP300, MYOD1, RPB1/POLR2A, AR, DSIF, and NELFE. CDK9-CCNT2 Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK9-CCNT2 Heterodimer protein, expressed by Sf9 insect cells , with tag free.
The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNT1 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK12-CCNT1, expressed by Sf9 insect cells , with N-His, N-GST, N-Flag labeled tag. ,
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8 Protein, Human (Sf9) is the recombinant human-derived CDK8, expressed by Sf9 insect cells , with tag Free labeled tag. The total length of CDK8 Protein, Human (Sf9) is 464 a.a.,
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8-CCNC-MED12 Protein, Human (Sf9) is the recombinant human-derived CDK8-CCNC-MED12 protein, expressed by Sf9 insect cells , with tag free.
The CDK8-CCNC-MED12 protein is an important component of the mediator complex, acting as a bridge for gene transcription regulation, transmitting information from gene-specific regulatory factors to RNA polymerase II. It is recruited to the promoter, assembles a preinitiation complex, and promotes transcription. CDK8-CCNC-MED12 Protein, Human (Sf9, GST, FLAG, His) is the recombinant human-derived CDK8-CCNC-MED12 protein, expressed by Sf9 insect cells , with N-6*His, N-Flag, N-GST labeled tag.
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