CDK Degrader
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CCNE1 degrader-2
0 ImagesCat. No.: HY-189497CAS No.: 3133169-21-5CCNE1 degrader-2 is an orally active CCNE1 degrader with a paDC50 of 7.7 nM. CCNE1 degrader-2 promotes the targeted degradation of Cyclin E1 protein. CCNE1 degrader-2 inhibits tumor cell proliferation and exerts antitumor activity in CDX in vivo models. CCNE1 degrader-2 is used in research on cancers such as ovarian cancer and breast cancer.
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PROTAC CDK4/6/9 degrader 1 prodrug
0 ImagesCat. No.: HY-178516PROTAC CDK4/6/9 degrader 1 prodrug is an orally active CDK4/CDK6/CDK9 PROTAC degrader prodrug. PROTAC CDK4/6/9 degrader 1 prodrug converts into PROTAC CDK4/6/9 degrader 1 (HY-178452). PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6 and CDK9. PROTAC CDK4/6/9 degrader 1 prodrug is applicable to the research of triple-negative breast cancer (prodrug modification moiety: Lauric acid (HY-Y0366); PROTAC moiety: PROTAC CDK4/6/9 degrader 1 (HY-178452)).
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PROTAC CDK9 degrader-12
0 ImagesCat. No.: HY-181231CAS No.: 3052648-82-2PROTAC CDK9 degrader-12 is a selective CDK9 PROTAC degrader with a DC50 of 23 nM. PROTAC CDK9 degrader-12 induces proteasome-dependent degradation of CDK9, blocks CDK9-mediated HIV-1 transcriptional elongation, and reduces HIV-1 RNA synthesis. PROTAC CDK9 degrader-12 is applicable to research related to HIV-1 infection.
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TR-213
0 ImagesCat. No.: HY-177743CAS No.: 2980502-40-5
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JHK-02-102-1
0 ImagesCat. No.: HY-184913JHK-02-102-1 is a selective CDK5 degrader derived from the regorafenib kinase inhibitor scaffold. JHK-02-102-1 recruits CRL4CRBN E3 ubiquitin ligase to induce ternary complex formation between CDK5 and CRBN, triggering ubiquitin-proteasome system-dependent degradation. JHK-02-102-1 achieves selectivity redirection from CDK6 to CDK5 via subtle PROTAC architecture modifications.
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SST0116CL1
0 ImagesCat. No.: HY-164399CAS No.: 1799802-29-1SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth. SST0116CL1 can be used for the study of leukemia, gastric and ovarian carcinoma.
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PROTAC CDK4/6/9 degrader 1
0 ImagesCat. No.: HY-178452CAS No.: 3064994-97-1PROTAC CDK4/6/9 degrader 1 is a CDK4/6/9 PROTAC degrader. PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6, and CDK9 in TNBC cells and inhibits TNBC cell proliferation. PROTAC CDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. PROTAC CDK4/6/9 degrader 1 can be used for the study of triple-negative breast cancer (TNBC). (Pink: CDK4/6/9 ligand (HY-168440), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-178512), E3 ligase ligand-linker conjugate (HY-178515)).
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CDK2 degrader 11
0 ImagesCat. No.: HY-187363CAS No.: 3121124-92-0CDK2 degrader 11 (Example 5) is a CDK2 degrader. CDK2 degrader 11 is applicable for cancer research.
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Cyclin K degrader 2
0 ImagesCat. No.: HY-177780Cyclin 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.
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Baleraciclideg
0 ImagesCat. No.: HY-187857CAS No.: 2883700-88-5Baleraciclideg is a Cyclin-dependent kinase degrader and antineoplastic.
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PROTAC CDK2-pRb degrader-1
0 ImagesCat. No.: HY-186132CAS No.: 3030276-48-0PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer).
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(R)-PROTAC CDK9 ligand-1
0 ImagesCat. No.: HY-115729ACAS No.: 2411021-95-7
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BSJ-03-123 (Standard)
0 ImagesCat. No.: HY-111556RCAS No.: 2361493-16-3BSJ-03-123 (Standard) is the analytical standard of BSJ-03-123 (HY-111556). This product is intended for research and analytical applications. BSJ-03-123 is a selective PROTAC degrader of CDK6. BSJ-03-123 degrades CDK6, thereby inhibiting Rb S780 phosphorylation and inducing G1 phase arrest, while remodeling cell cycle and transcriptional signaling, with no effect on CDK4-dependent cancer cells. BSJ-03-123 reduces CDK6 protein levels in mouse ovarian tissues, increases the proportion of primordial follicles, and induces granulosa cell apoptosis, without impairing the ability of oocytes to resume meiosis and mature to the MII stage. BSJ-03-123 alleviates uveitis by blocking the HDACs-CDK6/ID2 axis. BSJ-03-123 can be used in studies related to acute myeloid leukemia, mantle cell lymphoma and autoimmune uveitis.
