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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
25 Results for "
cyclin K degrader
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "cyclin K degrader" in MCE Product Catalog:
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(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 .
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2 Cited Publications
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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 .
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2 Cited Publications
Cat. No.: HY-18340A
CAS No.: 1786438-30-9
Synonyms: CR8, (R)-Isomer trihydrochloride
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(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 .
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1 Cited Publications
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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 .
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1 Cited Publications
Cat. No.: HY-162706
CAS No.: 2519823-37-9
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 .
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1 Cited Publications
Cat. No.: HY-W181530
CAS No.: 790245-61-3
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NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models .
Cat. No.: HY-163944
CAS No.: 3081311-94-3
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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 .
Cat. No.: HY-161168
CAS No.: 3055008-98-2
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Cyclin K degrader 1 is a molecular glue degrader derived from the pan-CDK inhibitor AT-7519 (HY-50940), with potent Cyclin K degrading activity and a DC50 of 21 nM. Cyclin K degrader 1 binds to CDK12, mediates the formation of a CDK12-DDB1 ternary protein complex, recruits the E3 ubiquitin ligase complex, and induces ubiquitination and proteasomal degradation of Cyclin K. Cyclin K degrader 1 can be used in the research of various Cyclin K-related diseases such as cancer .
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dCeMM4 is a Cyclin K Molecular glue degrader. dCeMM4 mediates the direct interaction between CDK12:cyclin K and the CRL4B ligase complex, thereby driving the ubiquitination and proteasomal degradation of Cyclin K. dCeMM4 induces Apoptosis without cell cycle phase-specific arrest. dCeMM4 exhibits synergistic activity with DNA damage inducers, and a correlation exists between Cyclin K degradation and cellular sensitivity. dCeMM4 can be used in studies related to T-cell malignancies .
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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 .
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LL-K8-22 is a dual degrader of CDK8 and cyclin C HyT, with DC50 values of 2.52 μM and 2.64 μM, respectively. LL-K8-22 inhibits phosphorylation of STAT1 Ser 727, phosphorylation of the C-terminal domain Ser 2/5 of RNA polymerase II, and phosphorylation of Rb. LL-K8-22 represses E2F- and MYC-driven transcriptional programs and exhibits antiproliferative effects. LL-K8-22 synchronously induces proteasome-dependent selective degradation of CDK8 and cyclin C without degrading CDK19, other CDK family members, or other cyclins. LL-K8-22 can be used in the research of triple-negative breast cancer and colon 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) .
Cat. No.: HY-179289
CAS No.: 3070379-34-6
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ZLY025 is a potent and orally active CCNK molecular glue degrader with an DC50 of 42.7 nM. ZLY025 exhibits broad-spectrum antiproliferative activity against various tumor cells with IC50 values ranging from 0.08 to 2.45 μM. ZLY025 can induce cells apoptosis and G1 phase arrest. ZLY025 can be used for the research of cancer, such as lung cancer .
Cat. No.: HY-156084
CAS No.: 2809353-52-2
LL-K9-3 is a selective CDK9-cyclin T1 HyT degrader, with DC50 values of 0.662 μM and 0.589 μM for CDK9 and Cyclin T1, respectively. LL-K9-3 lacks an E3 ligand moiety and induces polyubiquitination and proteasome-mediated synchronous degradation of CDK9 and cyclin T1 via a hydrophobic tag-mediated mechanism. LL-K9-3 downregulates the protein levels of androgen receptor (AR) and c-Myc, and exhibits antiproliferative and pro-apoptotic (apoptosis) activity in prostate cancer cells. LL-K9-3 can be used in studies related to prostate cancer .
Cat. No.: HY-177780
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Cyclin K degrader 2 is a molecular glue degrader of Cyclin K. By bridging CDK12 and DDB1, the receptor of the CRL4 E3 ligase, Cyclin K degrader 2 specifically induces the targeted degradation of Cyclin K within the CDK12-Cyclin K complex. Cyclin K degrader 2 can be used in studies related to acute myeloid leukemia .
Cat. No.: HY-171787A
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 .
Cat. No.: HY-W093149
CAS No.: 40248-63-3
Cat. No.: HY-160501
CAS No.: 3068546-95-9
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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 .
Cat. No.: HY-177743
CAS No.: 2980502-40-5
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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 .
Cat. No.: HY-150641
CAS No.: 3031561-92-6
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
