CDK Degrader

PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML.

CDK9 degrader-1 is a HyT-type CDK9 degrader that selectively induces protein degradation by recruiting ATG101 (with a DC₅₀ of 0.4073 μM in HCT116 cells). CDK9 degrader-1 recruits ATG101 to initiate the autophagy-lysosome pathway, forming LC3-containing autophagosomes that fuse with lysosomes to degrade CDK9. CDK9 degrader-1 mediates the degradation of Cyclin T1 via the same autophagy-lysosome pathway. CDK9 degrader-1 induces downstream phenotypic effects associated with CDK9 degradation. CDK9 degrader-1 can be used in the research of colorectal cancer (Blue: hydrophobic group; Pnk: CDK9 ligand (HY-50940); Black: linker (HY-N0420)).

CDK7 ligand 3 is a target protein ligand for CXJ2080 (HY-183070), which be used for the research of acute leukemia.

CST651 (PROTAC CDK4/6 degrader 34) is a selective cyclin-dependent kinase CDK4/6 PROTAC degrader with DC₅₀ values of 20 nM and 5.1 nM, respectively. CST651 recruits the VHL E3 ubiquitin ligase to mediate the ubiquitination and proteasomal degradation of CDK4/6. CST651 inhibits cancer cell proliferation and migration. CST651 can be used in research related to breast cancer, multiple myeloma, acute myeloid leukemia, and acute lymphoblastic leukemia.

CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC₅₀ of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia.

CDK2 degrader 8 is a selective cyclin-dependent kinase 2 (CDK2) degrader. CDK2 degrader 8 can be used in studies related to CDK2 degradation and HR⁺ HER2^- breast cancer.

CDK2 degrader 9 (compound 1) is a CDK2-targeting Molecular Glue with selectivity for GSPT1 and CDK1. CDK2 degrader 9 promotes the ubiquitination and degradation of CDK2 via the ubiquitin ligase pathway. CDK2 degrader 9 is applicable to research related to cancer, solid tumors and hematologic malignancies.

PROTAC CDK6 Degrader 2 (compound 48b), the active form of PROTAC CDK6 Degrader 1 (HY-180277), is a potent and selective PROTAC CDK6 degrader that binds strongly to KLHDC2 (K_D = 0.005 μM). PROTAC CDK6 Degrader 2 functions through a KLHDC2-dependent and ubiquitin-proteasome-mediated mechanism. PROTAC CDK6 Degrader 2 can be used for cancer research.

FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708).

PROTAC CDK4/6 degrader-2 is an orally active and selective PROTAC degrader that targets CDK4/6 degradation by recruiting cereblon. PROTAC CDK4/6 degrader-2 exhibits DC₅₀ values of 10.9 nM and 9.6 nM for CDK4 and CDK6, respectively. PROTAC CDK4/6 degrader-2 inhibits RB phosphorylation and cell cycle progression. PROTAC CDK4/6 degrader-2 is applicable for research on breast cancer and CDK4/6 inhibitor resistance.

PROTAC CDK9 degrader-13 is a selective CDK9 degrader acting via the ubiquitin-proteasome system. PROTAC CDK9 degrader-13 induces apoptosis in acute myeloid leukemia cells. PROTAC CDK9 degrader-13 suppresses tumor growth in vivo and has a defined safety profile. PROTAC CDK9 degrader-13 can be used for the research of acute myeloid leukemia.

PROTAC CDK9 degrader-14 is a CDK9 PROTAC degrader that recruits CRBN. PROTAC CDK9 degrader-14 efficiently degrades CDK9 and inhibits cell proliferation in solid tumors and hematological malignancies. PROTAC CDK9 degrader-14 can be used in research related to solid tumors, hematological malignancies and triple-negative breast cancer.

CDK12/13 ligand 2 is a potent CDK12 and CDK13 ligand. CDK12/13 ligand 2 can be used to synthesize YJ1206 (HY-168555).

CDK9 autophagic degrader 1 (Compound 28) is a ATTEC degrader that can be used to degrade CDK9 and also affects the levels of the associated Cyclin T1. CDK9 autophagic degrader 1 shows over 80% CDK9 inhibition rate at 100 nM. ( Pink: LC3B ligand (HY-168897); Black: linker (HY-W017758); Blue: target protein ligand (HY-10008); linker + target protein ligand (HY-168898))

Reziciclideg is a cyclin-dependent kinase (CDK) degrader and antitumor agent. Reziciclideg is applicable for cancer research.

CCNE1 degrader-1 (I-2) is a degrader targeting CCNE1. CCNE1 degrader-1 can be used in cancer-related research.

CDK2 degrader 10 is an orally active, cereblon-based molecular glue degrader targeting CDK2, with a DC₅₀ of 120 nM. CDK2 degrader 10 forms a ternary complex with cereblon and CDK2 via a non-canonical recruitment mode, thereby driving CDK2 degradation through the ubiquitin-proteasome system. CDK2 degrader 10 inhibits retinoblastoma protein phosphorylation, induces G1/S cell cycle arrest, and suppresses CDK2-dependent cell proliferation. CDK2 degrader 10 can be used in studies related to CDK2-dependent cancers.

CDK12 ligand-3 is a monovalent CDK12/13 and cyclin K molecular glue degrader. CDK12 ligand-3 recruits DDB1, a core component of CUL4-based E3 ubiquitin ligase complexes, to drive ubiquitination and degradation of its targets.

CDK9/CycT1 degrader-1 is an autophagy-anchored bifunctional degrader that mediates the degradation of the CDK9/cyclin T1 protein complex. CDK9/CycT1 degrader-1 binds both CDK9 and LC3B simultaneously to form a ternary complex, achieving target protein degradation via the autophagy-lysosome pathway. CDK9/CycT1 degrader-1 downregulates the protein levels of Mcl‑1 and c‑Myc and induces apoptosis. PROTAC CDK9/CycT1 Degrader-2 is applicable to cancer-related research.

JHK-02-108-2 is a PROTAC degrader targeting CDK6, with an EC₅₀ of 0.22 μM and a K_d of 1.9 μM. JHK-02-108-2 selectively promotes CRBN-dependent ubiquitination and proteasomal degradation of CDK6. JHK-02-108-2 induces sustained cell cycle arrest at the G₁ phase. JHK-02-108-2 reduces the phosphorylation level of retinoblastoma protein. JHK-02-108-2 can be used in research related to acute myeloid leukemia and glioblastoma.