STAT Degrader

AK-1690 is a selective PROTAC degrader targeting STAT6 (DC₅₀=1 nM) with a K_i of 6 nM against human STAT6. AK-1690 degrades STAT6 via the interaction of STAT6 with cereblon and a ubiquitin-like process. AK-1690 effectively depletes STAT6 protein in mouse liver and lung tissues, and is applicable to research related to leukemia, Hodgkin's lymphoma, follicular lymphoma, etc..

KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).

SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC₅₀: 0.5 μM), with IC₅₀ of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma.

STAT6 degrader-3 (Compound I-1) is a potent and selective STAT6 degrader with a DC₅₀ of <1 nM. STAT6 degrader-3 can be used in the research of Type 2 immune and allergic responses.

PROTAC STAT6 degrader-1 (Compound I-2) is a potent STAT6 PROTAC degrader with a DC₅₀ <1 nM. PROTAC STAT6 degrader-1 inhibits STAT6 activity with an IC₅₀ of <0.1 pM. PROTAC STAT6 degrader-1 can be used for inflammatory and cancers research, such as non-small cell lung cancer (NSCLC).

PROTAC STAT6 degrader-3 is a potent STAT6 PROTAC degrader with a DC₅₀ of less than 1 nM. PROTAC STAT6 degrader-3 can be used for research on allergic/inflammatory diseases and cancer.

PROTAC STAT3 degrader-3 is a STAT3 PROTAC degrader. PROTAC STAT3 degrader-3 recruits the E3 ubiquitin ligase CRBN and induces the degradation of STAT3 protein. PROTAC STAT3 degrader-3 inhibits the proliferation of malignant tumor cells. PROTAC STAT3 degrader-3 can be used for the research of non-small cell lung cancer and liver cancer.

SD-2301 is a selective STAT3 PROTAC degrader. SD-2301 induces STAT3 degradation without affecting the protein levels of other STAT family members (STAT1, STAT2, STAT4, STAT5, STAT6). SD-2301 exerts anti-tumor effects in B16F10-bearing mice. SD-2301 can be used for the study of cancer.

KT-333 ammonium (Compound A) is a molecular glues that degrades STAT3 protein. KT-333 ammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 ammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 ammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).

STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting Signal Transducer and Activator of Transcription 3 (STAT3). STAT3-D11-PROTAC-VHL exhibits anti-tumor activity with IC₅₀ values of 1335 nM and 1973 nM against HeLa and MCF-7 cells, respectively. STAT3-D11-PROTAC-VHL binds to the DNA-binding domain of STAT3 and recruits the E3 ligase VHL to form a ternary complex, leading to the ubiquitination of STAT3 and subsequent degradation by the proteasome. STAT3-D11-PROTAC-VHL also inhibits tumor cell growth, induces cell cycle arrest and apoptosis, and suppresses tumor immune evasion.

SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a K_i of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506).

STAT6 degrader-4 (Compound I-197) is a STAT6 degrading agent with a DC₅₀ value ranging from 1 to 10 μM. STAT6 degrader-4 can be used in cancer research.

PROTAC STAT6 degrader-7 is a STAT6 PROTAC degrader with an IC₅₀ of <0.1 μM. PROTAC STAT6 degrader-7 promotes ubiquitination and degradation of STAT6. PROTAC STAT6 degrader-7 can be used in cancer research.

PROTAC STAT6 degrader-8 is a STAT6 PROTAC degrader with a DC₅₀ value >0.1 μM and a DC_max value > 0.01 μM. PROTAC STAT6 degrader-8 has the potential for application in inflammation-related diseases.

KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).

STAT3 HiBiT degrader 1 is a STAT3 HiBiT degrader with a DC₅₀ of less than 0.05 μM in A549 cells.

PROTAC STAT6 degrader-5 is a PROTAC degrader that selectively targets STAT6. PROTAC STAT6 degrader-5 induces the degradation of STAT6 protein. PROTAC STAT6 degrader-5 can be used in inflammation and cancer research.

PROTAC STAT6 degrader-9 is a STAT6 PROTAC degrader with a DC₅₀ value >1 μM and a DC_max value > 0.1 μM. PROTAC STAT6 degrader-9 has the potential for application in inflammation-related diseases.

SD-965 is a selective STAT3 PROTAC degrader with a DC₅₀ of 0.14 μM. SD-965 promotes the ubiquitination and degradation of STAT3. SD-965 induces rapid, complete and persistent depletion of STAT3 protein. SD-965 induces tumor regression in mouse xenograft models of leukemia and lymphoma.

STAT6 degrader-1 (Compound 21) is a bifunctional molecular glue degrader of STAT6 that recruits E3 ubiquitin ligase. STAT6 degrader-1 induces proteasomal degradation of STAT6. STAT6 degrader-1 is applicable to the research of cancer, inflammatory diseases and colorectal cancer.