SWI/SNF Complex Degrader

PROTAC SMARCA2 degrader-21 (Compound I-5) is a PROTAC degrader for SMARCA, that degrades SMARCA2 with a DC₅₀ of 10-50 nM in A549 cell, and degrades SMARCA2 and SMARCA4 in MV411 with DC₅₀ of <1 nM and >100 nM, respectively.

PROTAC SMARCA2/4 degrader-6 is a SMARCA2 and SMARCA4 PROTAC degrader with a DC₅₀ of < 100 nM for both targets. It is applicable to cancer-related research.

(S,R,S)-AHPC-Me-amide-C9-acid is a E3 ligase ligand-linker conjugate, used for the synthesis of PROTAC SMARCA2 degrader-31 (HY-168234).

PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC₅₀ of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers.

PROTAC SMARCA2/4 degrader-36 is a bifunctional PROTAC degrader that degrades SMARCA2 and SMARCA4. PROTAC SMARCA2/4 degrader-36 hijacks the ubiquitin-proteasome system to mediate the degradation of SMARCA2/4 by binding to the VHL E3 ubiquitin ligase. PROTAC SMARCA2/4 degrader-36 downregulates SMARCA2/4 in tumor tissues in mouse xenograft models. PROTAC SMARCA2/4 degrader-36 can be used in studies related to non-small cell lung cancer.

PROTAC SMARCA2 degrader-25 is a PROTAC degrader targeting SMARCA2. PROTAC SMARCA2 degrader-25 is applicable to the research of smarca4-deficient cancers and multiple myeloma.

PROTAC SMARCA2/4-degrader-17 (Compound I-345) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-17 degrades SMARCA2 in A549 with DC₅₀ <100 nM, degrades SMARCA4 in MV411 with DC₅₀ <100 nM.

PROTAC SMARCA2/4 degrader-25 is a selective SMARCA2/SMARCA4 PROTAC degrader with selective anti-tumor activity. PROTAC SMARCA2/4 degrader-25 is activated by endogenous GSH, forms a ternary complex with SMARCA2 or SMARCA4 and VHL E3 ubiquitin ligase, and mediates degradation via the proteasome pathway. PROTAC SMARCA2/4 degrader-25 induces DNA damage and apoptosis, and inhibits cancer cell proliferation. PROTAC SMARCA2/4 degrader-25 is applicable to lung cancer-related research.

PROTAC SMARCA2/4 degrader-39 is a SMARCA2 and SMARCA4 PROTAC degrader with DC₅₀ values of < 0.1 nM and 0.1-<1 nM, respectively. PROTAC SMARCA2/4 degrader-39 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-39 is applicable to cervical cancer research.

PROTAC SMARCA2/4-degrader-29 (Compound I-279) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-29 degrades SMARCA2 in A549 with DC₅₀ <100 nM, degrades SMARCA4 in MV411 with DC₅₀ <100 nM.

PROTAC SMARCA2/4 degrader-32 is a SMARCA2/SMARCA4 PROTAC degrader. PROTAC SMARCA2/4 degrader-32 induces ubiquitination, proteasome-mediated degradation, and recruits the E3 ubiquitin ligase complex. PROTAC SMARCA2/4 degrader-32 can be used in cancer-related research.

PROTAC SMARCA2 degrader-35 (Compound 43) is a selective SMARCA2 PROTAC degrader with a DC₅₀ < 0.1 μM for SMARCA2. PROTAC SMARCA2 degrader-35 has anticancer activity and regulates cancer cell proliferation and growth through cell cycle arrest and DNA replication inhibition in SMARCA4-deleted cancer cells.

PROTAC SMARCA2 degrader-28 (Compound 158) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 with a DC₅₀ of 3 nM in HiBiT A549 cells.

PROTAC SMARCA2/4-degrader-19 (Compound I-412) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-19 degrades SMARCA2 in MV411 and in A549 with DC₅₀ <100 nM, degrades SMARCA4 in MV411 with DC₅₀ <100 nM.

PROTAC SMARCA2 degrader-26 (compound 45) is a potent SMARCA2 PROTAC degrader. PROTAC SMARCA2 degrader-26 induces SMARCA2 and SMARCA4 degradation in VCaP cells with the percent degradation of 94% and 57% for SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2 degrader-26 shows antiproliferative activity.

SMD-1087 is a VHL-recruiting SMARCA2 PROTAC degrader with a DC₅₀ of 8 nM. SMD-1087 induces ubiquitination and degradation of SMARCA2 via the proteasome pathway. SMD-1087 reduces PBRM1 protein levels, inhibits the growth of SMARCA4-deficient cancer cells, and suppresses tumor growth in mouse xenograft models. SMD-1087 can be used for research on SMARCA4-deficient human cancers, including lung cancer and melanoma.

PROTAC SMARCA2/4-degrader-31 (Compound I-280) is a degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-31 degrades SMARCA2 in A549 with DC₅₀ <100 nM, degrades SMARCA4 in MV411 with DC₅₀ <100 nM.

PROTAC SMARCA2 degrader-19 (Compound 46) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 in cell A549 and MV411 with a DC₅₀ < 100 nM. PROTAC SMARCA2 degrader-19 degrades SMARCA4 in cell MV411 with a DC₅₀ > 1000 nM.

PROTAC SMARCA2 degrader-20 (Compound I-40) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-20 has the potential for the research of cancer.

PROTAC SMARCA2/4-degrader-35 (Ex.43) is a SMARCA2/4 degrader with a DC₅₀ <2.5 nM