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Results for "

cyclin+K

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

9

Recombinant Proteins

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18340
    (R)​-​CR8
    1 Publications Verification

    CR8, (R)-Isomer

    		 Molecular Glues CDK Apoptosis Neurological Disease Cancer
    (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 .
    (R)​-​CR8
  • HY-144981
    HQ461
    1 Publications Verification

    		 CDK Molecular Glues Cancer
    HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death .
    HQ461
  • HY-162706
    BSJ-5-63
    1 Publications Verification

    		 PROTACs CDK Cancer
    BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. 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 (Pink: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078)) .
    BSJ-5-63
  • HY-163944
    LL-K12-18

    		DNA/RNA Synthesis Molecular Glues CDK Apoptosis RAD51 ATM/ATR PARP Cancer
    LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .
    LL-K12-18
  • HY-144971
    dCeMM2

    		Molecular Glues CDK Cancer
    dCeMM2 (Compound 2) is a molecular glue-type degrader that targets cyclin K. dCeMM2 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
    dCeMM2
  • HY-144977
    dCeMM4

    		Molecular Glues CDK Cancer
    dCeMM4 (Compound 5) is a molecular glue degrader. dCeMM4 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
    dCeMM4
  • HY-161168
    Cyclin K degrader 1

    		CDK Cancer
    Cyclin K degrader 1 (compound 40) is an AT7519 (HY-50940) based Cyclin K degrader with DC50 of 21 nM. Cyclin K degrader 1 has an affinity for cyclin K that is ~500-fold higher than its affinity for CDK12 .
    Cyclin K degrader 1
  • HY-18340A
    (R)-CR8 trihydrochloride
    1 Publications Verification

    CR8, (R)-Isomer trihydrochloride

    		 Molecular Glues CDK Apoptosis Neurological Disease Cancer
    (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 cyclin K .
    (R)-CR8 trihydrochloride
  • HY-144976
    dCeMM3

    		Molecular Glues CDK Cancer
    dCeMM3 (Compound 3) is a molecular glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .
    dCeMM3
  • HY-144691
    PP-C8

    		PROTACs CDK Cancer
    PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC) .
    PP-C8
  • HY-171787A
    PPA-037 TFA

    		CDK Cancer
    PPA-037 TFA is an orally active, highly potent and selective inhibitor of cyclin-dependent kinase 12 (CDK12). PPA-037 TFA induces the degradation of cyclin K (Cyclin K), enhancing antiproliferative effects on tumor cells. PPA-037 TFA is promising for research of cancers .
    PPA-037 TFA
  • HY-160501
    DS17

    		Molecular Glues CDK Cancer
    DS17 is a molecular glue that acts as a potent degrader of cyclin K, with an EC50 of 13 nM. DS17 plays an important role in cancer research .
    DS17
  • HY-177780
    Cyclin K degrader 2

    		Molecular Glues CDK Apoptosis Cancer
    Cyclin K degrader 2 is a molecular glucose degrading agent that targets the cyclin K protein. Cyclin K degrader 2 has inhibitory activity against CDK1 and CDK9. Cyclin K degrader 2 causes a decrease in RNA polymerase II Ser2 phosphorylation levels, downregulation of DNA damage response gene expression, accumulation of DNA damage, G1 phase arrest of the cell cycle, and apoptosis. Cyclin K degrader 2 can be used for cancer research .
    Cyclin K degrader 2
  • HY-108907
    SR-1277

    		Casein Kinase Cancer
    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/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer .
    SR-1277
  • HY-157297
    CDK-IN-13

    		CDK Cancer
    CDK-IN-13 (compound 32E) is a potent and selective inhibitor of CDK12/cyclinK with an IC50 of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines .
    CDK-IN-13
  • HY-177743
    TR-213

    		Molecular Glues CDK DNA/RNA Synthesis Cancer
    TR-213 is a potent molecular glue degrader that targets Cyclin K (CDK). TR-213 induces 91% and 56% decrease in CDK12 and Cyclin at 1 μM. TR-213 can inhibit RNA polymerase II activity and regulates alternative polyadenylation (APA) activity. TR-213 can be used for the research of cancer .
    TR-213
  • HY-150641
    CDK-IN-9

    		CDK Apoptosis DNA/RNA Synthesis Molecular Glues Cancer
    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 cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II .
    CDK-IN-9
  • HY-176790
    CDK12-Cyclin K ligand-1

    		Ligands for E3 Ligase Ligands for Target Protein for PROTAC Others
    CDK12-Cyclin K ligand-1 is a ligand of PROTAC degrader that binds to the E3 ligase. CDK12-Cyclin K ligand-1 can be used in the synthesis of PROTAC degrader such as PP-C8 (HY-144691) .
    CDK12-Cyclin K ligand-1
  • HY-176791
    CDK12-Cyclin K Ligand-Linker Conjugates 1

    		Target Protein Ligand-Linker Conjugates CDK Cancer
    CDK12-Cyclin K Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for CDK12-Cyclin K (HY-176790) and a PROTAC linker (HY-W244922), which recruits E3 ligases. CDK12-Cyclin K Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC PP-C8 (HY-144691) .
    CDK12-Cyclin K Ligand-Linker Conjugates 1
  • HY-171787
    PPA-037

    		CDK Cancer
    PPA-037 is an orally active, highly potent and selective inhibitor of cyclin-dependent kinase 12 (CDK12). PPA-037 induces the degradation of cyclin K (Cyclin K), enhancing antiproliferative effects on tumor cells. PPA-037 is promising for research of cancers .
    PPA-037
  • HY-177786
    CDK12 ligand-3

    		Molecular Glues CDK Cancer
    CDK12 ligand-3 is a molecular glucose degrading agent that targets the CDK12 protein (DC50 = 35 nM). CDK12 ligand-3 degrades CDK12, CDK13 and their regulatory subunit Cyclin K in a concentration dependent manner, and inhibits RNA polymerase II CTD (Ser2) phosphorylation. CDK12 ligand-3 exhibits potent anti proliferative activity against Jurkat cells. CDK12 ligand-3 can be used for research on cancers such as leukemia .
    CDK12 ligand-3
  • HY-136841
    SLM6

    		CDK Cancer
    SLM6 is a sangivamycin-like molecule. SLM6 is a CDK9 inhibitor. SLM6 inhibits CDK9/cyclin K 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 .
    SLM6

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