CDK6 Degrader

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.

YX-2-107 is a PROTAC (IC₅₀= 4.4 nM) that selectively degrades CDK6. YX-2-107 effectively inhibits RB phosphorylation and FOXM1 expression in vitro and inhibits the development of Ph⁺ ALL in rats. YX-2-107 can be used in the study of Ph chromosome-positive (Ph⁺) acute lymphoblastic leukemia (ALL).

PROTAC CDK4/6 degrader 1 is a CDK4/CDK6 PROTAC degrader, with DC₅₀ values of 10.5 nM and 2.5 nM, respectively. PROTAC CDK4/6 degrader 1 inhibits the proliferation of Jurkat cells (IC₅₀ = 0.18 μM), arrests the cell cycle at the G1 phase, and induces apoptosis. PROTAC CDK4/6 degrader 1 can be used for cancer research.

BSJ-02-162 (CDK4/6-IN-11) is a CDK4/CDK6 and IKZF1/IKZF3 degrader, with DC₅₀ values of 32 nM and 6.1 nM against CDK4 and CDK6, respectively; its IC₅₀ ranges from 1 to 50 nM. BSJ-02-162 induces G1-phase cell cycle arrest, reduces phosphorylated retinoblastoma protein levels, and exerts antiproliferative activity in mantle cell lymphoma cells. BSJ-02-162 is applicable to research related to mantle cell lymphoma.

LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC₅₀ of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer.

PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research.

LO-3-63 is a CDK4/CDK6 degrader. LO-3-63 induces proteasome-dependent degradation of CDK4/6 via CUL4^DCAF16-dependent interaction.

WWZ-11-098 is a selective CDK6 PROTAC degrader with DC₅₀ of 2.6 nM. WWZ-11-098 induces degradation of CDK6 in a CRBN-dependent manner, while sparing CDK1, CDK2, CDK4, and CDK9. WWZ-11-098 induces apoptosis, G1-S cell cycle arrest and shows anti-proliferative activity in cancer cells. WWZ-11-098 exhibits antitumor efficacy in a xenograft model without signs of toxicity. WWZ-11-098 can be used for the research of leukemia.

PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC₅₀ of 0.037 μM. PROTAC CDK6 Degrader 1 exhibits selectivity over CDK4 (DC₅₀ > 10 μM). PROTAC CDK6 Degrader 1 induces G0/G1 cell-cycle arrest and apoptosis through inhibition of CDK6 downstream signaling. PROTAC CDK6 Degrader 1 reduces tumor burden and CDK6 levels in a MOLM-14 xenograft mouse model. PROTAC CDK6 Degrader 1 can be used for CDK6-driven cancers research, such as acute myeloid leukemia (AML).

PROTAC FLT3/CDKs degrader-1 is a PROTAC degrader targeting CDKs and FLT3. PROTAC FLT3/CDKs degrader-1 degrades CDK2, CDK4, CDK6, CDK9 and FLT3 proteins via a ubiquitin-proteasome-dependent bivalent mechanism, with a DC₅₀ of 18.73 nM against CDK2. PROTAC FLT3/CDKs degrader-1 promotes myeloid cell differentiation. PROTAC FLT3/CDKs degrader-1 inhibits leukemia cell proliferation. PROTAC FLT3/CDKs degrader-1 can be used for the research of acute myeloid leukemia.

TMX-2138 is a CDK PROTAC degrader, with IC₅₀ values against different targets as follows: CDK1 (IC₅₀ = 8.7 nM), CDK2 (IC₅₀ = 10.9 nM), CDK5 (IC₅₀ = 7.0 nM), CDK4 (IC₅₀ = 901.0 nM), CDK6 (IC₅₀ = 465.0 nM), CDK7 (IC₅₀ = 286.0 nM), and CDK9 (IC₅₀ = 25.7 nM). TMX-2138 promotes the ubiquitination of CDK and induces its degradation via the proteasomal pathway. TMX-2138 can be used in ovarian cancer research.

CDK6 ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs) that targets CDK6. CDK6 ligand-3 can be used to synthesize the PROTAC JHK-02-108-2 (HY-184910).

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.

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).

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.

PROTAC 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)).

PROTAC 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)).

BSJ-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.