Catalog No.
Product Name
Application
Product Information
Citations
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Ligands for Target Protein for PROTAC
CBP/p300 ligand 10 is a selective ligand for the CBP/p300 proteins, facilitating their targeted degradation. This compound serves as a valuable component for the development of PROTACs, specifically enabling the synthesis of CBP/p300 Degrader-2. Its utility in research applications includes studies focused on cellular signaling pathways and potential therapeutic interventions in diseases associated with dysregulated CBP/p300 activity. -
ZBTB7A/WIZ Dual Molecular Glue Degrader
BMS-986470 is a dual molecular glue degrader that targets ZBTB7A and WIZ through modulation of the CRBN E3 ligase. This compound demonstrates potent induction of γ-globin, making it a valuable tool for studying hemoglobin disorders. BMS-986470 holds significant potential for research applications related to sickle cell disease (SCD), facilitating investigations into therapeutic strategies and molecular mechanisms underlying the condition. -
Molecular Glue
TCIP3 is a bivalent molecular glue that targets p300/CBP and BCL6. By redirecting p300 and CBP, TCIP3 activates programmed cell death genes that are typically suppressed by the oncogenic driver BCL6, making it a valuable tool for investigating diffuse large B cell lymphomas (DLBCLs). Importantly, TCIP3 demonstrates no toxicity to non-transformed tonsillar lymphocytes or fibroblasts, ensuring the safety of experimental applications. -
WIZ Molecular Glue
WIZ degrader 8 is a selective degrader targeting the transcription factor WIZ, promoting the degradation of WIZ and subsequently inducing the expression of fetal hemoglobin (HbF). This compound has significant potential for research applications related to sickle cell disease, as it may serve as a therapeutic strategy to modulate HbF levels and alleviate disease symptoms. -
p300 PROTAC Degrader
BT-O2C is a selective p300 PROTAC degrader that effectively reduces p300 levels in HAP1 cells. It exhibits significant cytotoxicity in CIC:DUX4 sarcoma cell lines, with IC50 values ranging from 152 to 221 nM, and notably decreases the expression of target genes associated with CDS, such as ETV1, ETV4, and ETV5. This compound serves as a valuable tool for research in cancer biology, facilitating studies on p300's role in oncogenic processes. -
PCAF/GCN5 PROTAC Degrader
GSK699 is a PROTAC degrader targeting PCAF/GCN5, promoting their ubiquitination and subsequent proteasomal degradation. This compound effectively inhibits the production of key cytokines and chemokines, such as interleukin-6 (IL-6) and CXCL1/GROα, thus demonstrating significant anti-inflammatory properties. GSK699 is suitable for investigations related to inflammatory diseases and other conditions modulated by these target proteins. -
BRD4/CBP/p300 PROTAC Degrader
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader that specifically targets BRD4, CBP, and p300, achieving DC50 values of 8.8 pM, 6.55 nM, and 1.05 nM, respectively. This compound promotes CRBN- and proteasome-mediated degradation of BRD4 and CBP/p300, leading to the downregulation of c-Myc and acetyl-H3K27, and inducing apoptosis. It exhibits significant antiproliferative and antitumor effects, demonstrated by tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 is a valuable tool for research focused on prostate and colorectal cancer. -
HDAC PROTAC Inhibitor
JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor that targets HDAC1, HDAC2, and HDAC3 for ubiquitination and proteasomal degradation via VHL E3 ligase recruitment. This compound demonstrates significant anticancer activity by reducing the viability of colon cancer cells and inducing apoptosis. Additionally, JPS016 activates the PINK1/Parkin-mediated mitochondrial autophagy pathway, enhancing cardiomyocyte viability, alleviating mitochondrial damage, and decreasing mitochondrial ROS production. It is valuable for research into colon cancer and sepsis-related cardiac dysfunction. -
PROTAC HDAC6 Degrader
HDAC6 Degrader-3 is a selective inhibitor that promotes the degradation of histone deacetylase 6 (HDAC6) through ternary complex formation and the ubiquitin-proteasome pathway, exhibiting a DC50 value of 19.4 nM. With IC50 values of 4.54 nM for HDAC6 and 0.647 μM for HDAC1, it effectively induces significant hyperacetylation of α-tubulin. This compound is valuable for research applications focused on neurodegenerative diseases and cancer, where modulation of HDAC6 activity may play a critical role. -
PROTAC HDAC Degrader
HD-TAC7 is a highly effective PROTAC HDAC degrader, specifically targeting histone deacetylases HDAC1, HDAC2, and HDAC3 with IC50 values of 3.6 μM, 4.2 μM, and 1.1 μM, respectively. This compound has demonstrated the ability to reduce NF-κB p65 levels in RAW 264.7 macrophages. HD-TAC7 is suitable for research applications focused on inflammatory diseases, including asthma and chronic obstructive pulmonary disease (COPD). -
PROTAC HDAC Degrader
JPS036 is a benzamide-based HDAC degrader that operates through the Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC) mechanism. This compound selectively degrades class I histone deacetylases (HDAC1 and HDAC2), demonstrating significant biological activity by promoting the expression of differentially expressed genes and enhancing apoptosis in HCT116 cells. JPS036 serves as a valuable research tool for studying the roles of HDACs in cellular processes and disease models. -
EZH2 Degrader
PROTAC EZH2 Degrader-3 (compound ZJ-20) specifically targets and degrades the EZH2 protein through a proteolysis-targeting chimera (PROTAC) mechanism. This compound demonstrates potent inhibition of EZH2 expression as well as a significant reduction in other PRC2 subunits and H3K27me3 levels. Additionally, PROTAC EZH2 Degrader-3 exhibits anti-proliferative effects, inducing cell cycle arrest in the G0-G1 phase and promoting apoptosis in cancer cells, making it valuable for research in cancer therapeutics and epigenetic regulation. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-9 is an orally active PROTAC that selectively degrades EZH2 via the ubiquitin-proteasome pathway. By downregulating PRC2 core subunits and inhibiting H3K27me3, it effectively reverses PRC2-mediated gene silencing and disrupts EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 demonstrates potent antiproliferative effects on various cancer cell lines, inducing cell cycle arrest and apoptosis. This reagent is valuable for research focused on leukemia, lymphoma, and non-small cell lung cancer. -
CARM1 PROTAC Degrader
CARM1 degrader-1 is a selective PROTAC degrader targeting CARM1, exhibiting a DC50 value of 8.1 nM. It effectively degrades CARM1 through a VHL- and proteasome-mediated mechanism, leading to a reduction in the methylation levels of CARM1 substrates in various cell-based assays. Additionally, CARM1 degrader-1 demonstrates the ability to inhibit cancer cell migration, making it a valuable tool for investigating mechanisms in breast cancer research. -
Ligands for Target Protein for PROTAC
Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH is a ligand specifically designed for EZH2, functioning as a key component in PROTAC technology by recruiting E3 ligases. This compound demonstrates potential biological activity in targeted protein degradation, particularly in the context of lymphoma research. Its unique structure allows for the exploration of novel therapeutic strategies aimed at modulating EZH2 activity and its downstream effects in cancer biology. -
PROTAC Linker
MAK683-CH2CH2COOH is a PROTAC linker that specifically binds to embryonic ectoderm development protein (EED). This compound is instrumental in facilitating targeted protein degradation when paired with a VHL ligand for E3 ubiquitin ligase. Research applications include the development of PROTAC EED degrader-1 and PROTAC EED degrader-2, making it a valuable tool for studying EED-related pathways and therapeutic interventions. -
PROTAC Glutathione Peroxidase Degrader
NC-R17 is a non-covalent degrader targeting Glutathione Peroxidase 4 (GPX4) through the PROTAC mechanism, designed to induce ferroptosis in cancer cells. Exhibiting significant antitumor activity, NC-R17 facilitates the targeted degradation of GPX4, contributing to research in cancer biology and therapeutic strategies. The compound combines a Demethyl-RSL3 ligand for GPX4 with an E3 ubiquitin ligase ligand derived from Lenalidomide, connected by a specific PROTAC linker to enhance its biological activity. -
GPX4 PROTAC Degrader
PROTAC GPX4 degrader-4 selectively targets GPX4, functioning as a PROTAC degrader with a DC50 of 5.32 nM. This compound effectively inhibits the proliferation of RT4, T24, and J82 bladder cancer cell lines, exhibiting IC50 values of 0.09, 2.97, and 7.58 μM, respectively. PROTAC GPX4 degrader-4 promotes the accumulation of lipid reactive oxygen species (ROS) and triggers ferroptosis in T24 and RT4 cells. Additionally, it demonstrates significant antitumor efficacy in a T24 tumor-bearing BALB/c nude mouse model, making it a valuable tool for bladder cancer research. -
Molecular Glues
Lenalidomide hemihydrate functions as a molecular glue through its activity as an immunomodulator. This compound selectively binds to the ubiquitin E3 ligase cereblon (CRBN), leading to the ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 complex. Lenalidomide hemihydrate is effective in inhibiting the proliferation of mature B-cell lymphomas, including multiple myeloma, and promotes the release of IL-2 from T cells, making it a valuable tool in cancer research. -
NEK7 Molecular Glue Degrader
NEK7 degrader-3 is an orally active NEK7 molecular glue degrader with a DC50 of 33.1 nM, which effectively mediates the interaction between NEK7 and the E3 ligase cereblon, leading to the proteasomal degradation of NEK7. This degradation process attenuates NLRP3 inflammasome-mediated inflammatory responses, resulting in the inhibition of caspase-1 activity and the release of pro-inflammatory cytokines IL-1β, IL-1α, and IL-18. NEK7 degrader-3 demonstrates significant anti-inflammatory effects in LPS-induced neuroinflammation mouse models, serving as a valuable tool for research focused on neuroinflammation. -
Molecular Glue
ABT-002 is a molecular glue degrader that targets GSPT1 and NEK7, enhancing the ubiquitin-proteasome system's ability to degrade these proteins. This compound is the active metabolite of ABS-752 and demonstrates potential in the research of hepatocellular carcinoma (HCC). Its unique mechanism of action makes it a valuable tool for elucidating cellular pathways and therapeutic strategies in cancer biology. -
GSPT1/NEK7 Degrader
ABS-752 is a potent molecular glue degrader targeting GSPT1 and NEK7. It demonstrates significant cytotoxicity by reducing the protein levels of both GSPT1 and SALL4, along with NEK7. As a prodrug, ABS-752 is activated by monoamine oxidase, VAP-1, into an aldehyde intermediate and further converted to its active form, ABT-002. This compound has promising applications for research into hepatocellular carcinoma. -
GSPT1 Molecular Glue
ABS-752 hydrochloride is a prodrug that targets GSPT1 through CRBN modulation, functioning as a molecular glue. It effectively degrades GSPT1 and NEK7, without forming ternary complexes with CRBN and neosubstrates. The compound is activated by the enzyme VAP-1, converting it into an aldehyde intermediate and subsequently yielding the active molecule, ABT-002. ABS-752 is utilized in research focused on hepatocellular carcinoma (HCC) and related therapeutic pathways. -
H-PGDS PROTAC Degrader
PROTAC(H-PGDS)-7 is a targeted protein degradation agent that selectively degrades hematopoietic prostaglandin D synthase (H-PGDS). With a DC50 value of 17.3 pM, it demonstrates potent biological activity in modulating the levels of H-PGDS. This compound is valuable for research applications involving the role of H-PGDS in inflammatory processes and may assist in elucidating therapeutic strategies for related diseases. -
H-PGD PROTAC Degrader
PROTAC(H-PGDS)-8 is a targeted protein degradation compound that specifically degrades hematopoietic prostaglandin D synthase (H-PGDS) with an IC50 of 0.14 μM. This PROTAC molecule facilitates the ubiquitination and subsequent proteasomal degradation of H-PGDS, making it a valuable tool for investigating the role of H-PGDS in various biological processes. Research applications include studies on inflammation, pain mechanisms, and other pathophysiological conditions where H-PGDS is implicated. -
PROTAC Degrader
RP03707 is a potent PROTAC degrader targeting KRASG12D. By forming a ternary complex with KRASG12D and the CRBN E3 ligase, RP03707 facilitates the ubiquitination and subsequent proteasomal degradation of KRASG12D. This compound demonstrates significant inhibitory effects on the growth of KRASG12D-positive tumor cells, making it an essential tool for research in cancer biology and targeted therapy development. -
K-Ras PROTAC Degrader
PROTAC K-Ras Degrader-3 is a powerful PROTAC compound designed to target and degrade K-Ras, demonstrating a DC50 of ≤ 1 nM in SW620 KRAS G12D cells and a GI50 of ≤ 10 nM for inhibiting SW620 3D cell growth. This compound is particularly valuable in cancer research, especially for studying non-small-cell lung cancer (NSCLC). Its unique design incorporates a K-RAS ligand, a Cereblon ligand, and a linker, facilitating targeted degradation and offering insights into K-Ras-related pathways. -
Molecular Glues
PRLX-93936 is a molecular glue that targets the TRIM21 ubiquitin ligase to facilitate the degradation of nuclear pore complexes. By binding to TRIM21 and forming a ternary complex with TRIM21 and NUP98, this compound mediates ubiquitination and proteasomal degradation of NUP98 and related proteins. PRLX-93936 induces apoptosis in cancer cells, reduces the levels of short-lived cytoplasmic mRNA transcripts, and inhibits the activated Ras signaling pathway. It demonstrates significant antitumor activity in mouse models, particularly for pancreatic cancer and multiple myeloma, making it a valuable tool for cancer research. -
KRAS G12D Molecular Glue Degrader
IPS-06061 is a molecular glue degrader that targets the KRAS G12D mutant through the formation of a ternary complex with CRBN. This compound effectively degrades KRAS G12D with a DC50 value of less than 500 nM, demonstrating significant anti-tumor efficacy. It serves as a valuable tool for research into targeted therapies for cancers driven by KRAS mutations. -
KRAS(on) PROTAC Degrader
ACBI-4 is a selective PROTAC degrader targeting the active state of KRAS (KRAS(on)). This compound exhibits significant anti-proliferative effects and effectively degrades various KRAS mutants, including KRASG12R, in cancer cell models. ACBI-4 is valuable for research applications focused on understanding KRAS-mediated signaling pathways and developing targeted cancer therapies. -
Pan-KRAS PROTAC Degrader
PROTAC pan-KRAS degrader-1 targets pan-KRAS mutations, facilitating the degradation of various KRAS variants, including G12D, G12C, G12V, and G13D. This compound exhibits potent activity against the G12D mutation in AGS cells, achieving a DC50 of 1.1 nM and a maximum degradation efficacy (Dmax) of 95%. PROTAC pan-KRAS degrader-1 is a valuable tool for investigating diseases associated with KRAS mutations and amplifications, particularly in cancer types such as breast, bladder, and gastric cancer. -
STING Molecular Glue
NVS-STG2 is a molecular glue that targets the STING receptor by binding to the interstitial regions of adjacent STING dimers, thereby enhancing STING signaling. This compound promotes the activity of cGAMP, leading to the formation of larger and more stable oligomers, which amplifies the immune response. NVS-STG2 has demonstrated significant antitumor effects in preclinical animal models, making it a valuable tool for cancer immunotherapy research. -
STING PROTAC Degrader
PROTAC STING degrader-3 is a potent STING PROTAC degrader that operates through the ubiquitin-proteasome pathway, exhibiting a DC50 of 0.62 μM. This compound facilitates STING degradation, resulting in the inhibition of STING/TBK1/NF-κB signaling, thereby exerting notable anti-inflammatory effects. Additionally, PROTAC STING degrader-3 demonstrates renal protective properties and serves as a valuable tool for investigating acute kidney injury (AKI). -
PROTAC STING Degrader
PROTAC STING Degrader-2 is a targeted protein degrader that specifically induces the degradation of the Stimulator of Interferon Genes (STING) through a covalent interaction with STING and an E3 ubiquitin ligase. With a DC50 value of 0.53 μM, this compound facilitates the study of STING's biological functions, particularly in the context of autoinflammatory and autoimmune diseases. This reagent is instrumental for researchers exploring the therapeutic potential and role of STING in immune regulation. -
cGAS PROTAC Degrader
PROTAC cGAS degrader-1 is a selective degrader targeting cGAS through a proteolysis-targeting chimera (PROTAC) mechanism. It effectively induces proteasome-mediated degradation of cGAS, leading to the inhibition of the cGAS signaling pathway and a reduction in double-stranded DNA-induced cGAS activation in both human and mouse cell models. This compound is particularly relevant for research applications in inflammatory diseases such as ulcerative colitis. -
p300/CBP Degrader
MJP6412 is a selective degrader of the histone acetyltransferases p300 and CBP, exhibiting DC50 values of 1.6 nM and 1.2 nM, respectively. This compound effectively induces degradation of these proteins, thereby modulating acetylation levels in cells. MJP6412 is particularly relevant in cancer research, providing insights into the role of p300 and CBP in oncogenic processes and potential therapeutic interventions. -
PROTAC KDM5B Degrader
GT-653 is a PROTAC degrader targeting lysine-specific demethylase 5B (KDM5B). It efficiently induces degradation of KDM5B by 68.35% at a concentration of 10 μM through a ubiquitin proteasome-dependent mechanism. This compound elevates H3K4me3 levels and activates type-I interferon signaling pathways in prostate cancer cells, specifically in the 22RV1 cell line. Research applications include studying KDM5B's role in cancer biology and evaluating potential therapeutic strategies that involve epigenetic modulation. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-12 is a CRBN-recruiting PROTAC designed to selectively degrade the EZH2 protein, exhibiting an IC50 of 3.90 nM for EZH2 and an IC50 of 5.24 μM for EZH1. This compound facilitates targeted protein degradation, making it a valuable tool for research focused on epigenetic regulation and cancer biology. Its ability to modulate the expression of key oncogenic factors positions it as a significant reagent for therapeutic investigations targeting EZH2-dependent pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-24 is an innovative molecule designed to target EZH2 by utilizing a PROTAC-mediated degradation mechanism. This compound exhibits potent EZH2 methyltransferase inhibitory activity, facilitating the selective degradation of the EZH2 protein. Research applications include studies on epigenetic regulation and therapeutic strategies for cancers with aberrant EZH2 activity. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-30 is a PROTAC protein degrader specifically designed to target the enhancer of zeste homolog 2 (EZH2) with an IC50 of 6.22 μM in SU-DHL-6 cells. This compound is instrumental in research applications focusing on diffuse large B-cell lymphoma by promoting the degradation of EZH2 and thereby modulating epigenetic regulation. The inclusion of ligands for both EZH2 and MDM2, coupled with a linker, facilitates targeted protein degradation and offers a valuable tool for investigating therapeutic strategies in cancer biology. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-43 is a targeted PROTAC protein degrader that specifically degrades the EZH2 protein, exhibiting an IC50 of 21.73 μM in SU-DHL-6 cells. This compound is valuable for investigating the role of EZH2 in lymphoma research and understanding its mechanistic function in histone methylation. The dual ligand design incorporates a histone methyltransferase ligand and a VHL ligand, promoting efficient substrate recognition and recruitment for proteasomal degradation. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-17 is a selective protein degrader that targets the enhancer of zeste homolog 2 (EZH2). This compound demonstrates significant antiproliferative activity, with an IC50 of 18.32 μM in lymphoma cell lines. PROTAC EZH2 Degrader-17 is a valuable tool for investigating EZH2-related pathologies and provides insights into the therapeutic potential of protein degradation in cancer research. -
EZH2 Ligand
EZH2 ligand-3 functions as a ligand targeting the Enhancer of Zeste Homolog 2 (EZH2) protein. This compound plays a crucial role in the synthesis of PROTAC EZH2 Degrader-35, facilitating the selective degradation of EZH2 in cellular models. It is valuable for research applications focused on epigenetic regulation and targeted protein degradation strategies. -
EZH2 PROTAC
PROTAC EZH2 Degrader-26 is a targeted proteolysis-targeting chimera (PROTAC) designed to specifically degradation of the enhancer of zeste homolog 2 (EZH2). This compound demonstrates a potent inhibitory activity with an IC50 of 5.80 nM against EZH2, alongside micromolar-level activity against EZH1, with an IC50 of 0.06 μM. PROTAC EZH2 Degrader-26 is suitable for research applications involving epigenetic regulation, cancer biology, and studies aimed at understanding histone methylation processes. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-39 is a targeted PROTAC that effectively degrades the EZH2 protein, exhibiting an IC50 of 61.00 nM. This compound functionally inhibits the methyltransferase activity of EZH2, making it an important tool for studying the biological implications of EZH2 modulation. Its applications include cancer research and epigenetic regulation studies, contributing to advancements in targeted therapy development. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-15 is a targeted degrader that specifically interacts with the EZH2 protein via a proteolysis-targeting chimera (PROTAC) mechanism. This compound effectively inhibits the methyltransferase activity of EZH2, leading to its degradation and resulting in alterations to histone methylation patterns. It serves as a valuable tool for research applications focused on epigenetic regulation, cancer biology, and therapeutic strategies aimed at EZH2 modulated pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-10 is a Proteolysis Targeting Chimeras (PROTAC) compound designed to selectively degrade the enhancer of zeste homolog 2 (EZH2). By facilitating the ubiquitination and subsequent proteasomal degradation of EZH2, this compound exhibits potential as an innovative therapeutic approach for cancer research. Its mechanism involves a specific ligand for EZH2 and a cereblon ligand, linked together to enhance degradation efficiency, making it a valuable tool for investigating EZH2-related oncogenic pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-35 is a proteolysis-targeting chimera (PROTAC) specifically designed to degrade the Enhancer of Zeste Homolog 2 (EZH2) protein, exhibiting a binding affinity (Ka) of 16.19 nM. This compound demonstrates significant antiproliferative activity against triple-negative breast cancer cells while maintaining minimal cytotoxicity toward normal human epithelial, hepatic, and renal cells. PROTAC EZH2 Degrader-35 is a valuable tool for studying the role of EZH2 in cancer biology and has potential applications in therapeutic research focused on triple-negative breast cancer. -
EZH2 PROTAC
PROTAC EZH2 Degrader-27 is a potent EZH2 PROTAC inhibitor with an IC50 of 4.00 nM, specifically designed to target the SET domain of the EZH2 methyltransferase. By engaging in targeted protein degradation, this compound effectively inhibits methyltransferase activity, leading to downregulation of histone methylation. Research applications include studies on epigenetic regulation and potential therapeutic strategies targeting EZH2 in various cancers. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-13 is a targeted proteolysis-targeting chimera (PROTAC) designed to selectively degrade Enhancer of Zeste Homolog 2 (EZH2) with an IC50 of 2.70 nM. This compound exhibits potent antiproliferative effects in various cancer cell lines, making it a valuable tool in cancer research. PROTAC EZH2 Degrader-13 facilitates investigations into the role of EZH2 in tumorigenesis and therapeutic resistance, providing insights for the development of innovative cancer treatments.
