Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC K-Ras Degrader
PROTAC K-Ras Degrader-1 (Compound 518) is a cereblon-based PROTAC that selectively degrades K-Ras, achieving ≥70% degradation efficiency in SW1573 cells. It serves as a valuable tool for studying K-Ras-driven signaling pathways and potential therapeutic strategies in cancer research. -
SMARCA2/SMARCA4/PBRM1 Degrader
ACBI1 is a potent and cooperative PROTAC degrader targeting SMARCA2, SMARCA4, and PBRM1, with DC₅₀ values of 6 nM, 11 nM, and 32 nM, respectively. It exhibits strong anti-proliferative activity and induces apoptosis, making it a valuable tool for studying chromatin remodeling and cancer therapeutics. -
Halo PROTAC degrader
HaloPROTAC-E is a potent and selective PROTAC designed to degrade Halo-tagged endoplasmic reticulum-localized proteins, including SGK3 and VPS34, with a DC₅₀ of 3–10 nM. It effectively induces degradation of endogenous VPS34 complexes (VPS34, VPS15, Beclin1, and ATG14) when Halo-tagged, leading to inhibition of autophagy. HaloPROTAC-E is a valuable tool for conditional protein degradation and autophagy research. -
PROTAC CDK4 Degrader
BSJ-04-132 is a potent and selective Ribociclib-based PROTAC degrader targeting CDK4, constructed using ligands for cereblon and CDK. It exhibits IC₅₀ values of 50.6 nM for CDK4/D1 and 30 nM for CDK6/D1, while sparing CDK6 and IKZF1/3 from degradation. BSJ-04-132 demonstrates anti-cancer activity and is a valuable tool for cell cycle and oncology research. -
PROTAC CDK4/6 Degrader
BSJ-03-204 is a potent and selective PROTAC degrader targeting CDK4 and CDK6, constructed by linking Palbociclib to a cereblon ligand. It exhibits IC₅₀ values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1, without inducing degradation of IKZF1 or IKZF3. BSJ-03-204 demonstrates strong anti-cancer activity and is a valuable tool for cell cycle and oncology research. -
multi-kinase PROTAC degrader
TL12-186 is a cereblon-dependent PROTAC degrader with broad-spectrum activity against multiple kinases, including CDKs, BTK, FLT3, Aurora kinases, TEC, ULK, and ITK. It inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC₅₀ values of 73 nM and 55 nM, respectively, making it a valuable tool for studying kinase-driven signaling pathways and cancer biology. -
PROTAC CDK4/6 degrader
XY028-140 (MS140) is a highly potent and selective dual-function compound that acts as both a CDK4/6 kinase inhibitor and a PROTAC degrader. By combining kinase inhibition with targeted protein degradation, MS140 provides an effective approach for disrupting CDK4/6-mediated cell cycle regulation, making it a valuable tool for cancer research. -
estrogen receptor PROTAC protein degrader
Vepdegestrant (ARV-471) is an orally bioavailable PROTAC designed to target and degrade the estrogen receptor (ER). It is being developed for the treatment of patients with locally advanced or metastatic ER+/HER2− breast cancer, offering a novel approach to overcome endocrine resistance through targeted ER degradation. -
EZH2 PROTAC Degrader
MS177 is a fast-acting and effective PROTAC degrader targeting EZH2. It comprises a cereblon (CRBN) ligand, a linker, and the potent EZH2 enzymatic inhibitor C24 (IC₅₀: 12 nM). MS177 efficiently depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes, leading to inhibition of leukemia cell proliferation, induction of apoptosis, and cell cycle arrest. It is a valuable tool for epigenetic and cancer research. -
PROTAC-based EZH2 Degrader
MS1943 is an orally active, PROTAC-based selective degrader of EZH2 that effectively reduces cellular EZH2 levels. It exhibits strong anticancer activity, showing cytotoxic effects in various triple-negative breast cancer (TNBC) cell lines while sparing normal cells. MS1943 maintains high potency in inhibiting EZH2 methyltransferase activity (IC₅₀ = 120 nM) and demonstrates high selectivity for EZH2, making it a promising candidate for epigenetic and cancer research. -
androgen receptor (AR) PROTAC degrader
Bavdegalutamide (ARV-110) is an orally active and highly specific PROTAC degrader targeting the androgen receptor (AR). It induces ubiquitination and proteasomal degradation of AR, offering a novel therapeutic approach for AR-driven diseases such as prostate cancer. -
FKBP12F36V degrader
dTAG-13 is a PROTAC-based heterobifunctional degrader that selectively targets FKBP12^F36V fused in-frame to a protein of interest. By engaging both FKBP12^F36V and the cereblon (CRBN) E3 ligase, dTAG-13 induces efficient and selective degradation of FKBP12^F36V-tagged proteins, making it a valuable tool for conditional protein knockdown studies. -
Androgen Receptor (AR) degrader
ARCC-4 is a low-nanomolar PROTAC degrader targeting the androgen receptor (AR), with a DC₅₀ of 5 nM. Based on enzalutamide and incorporating a von Hippel-Lindau (VHL) E3 ligase ligand, ARCC-4 efficiently degrades both wild-type and clinically relevant AR mutants linked to resistance to antiandrogen therapy. It outperforms enzalutamide in potency and degradation efficacy, making it a promising candidate for advanced prostate cancer research. -
SMARCA2/SMARCA4/PBRM1 Degrader
AU-24118 is an orally bioavailable PROTAC degrader targeting the mSWI/SNF chromatin remodeling complex ATPases SMARCA2 and SMARCA4, as well as PBRM1. It offers a powerful approach for modulating epigenetic regulation and holds promise for the treatment of cancers driven by alterations in SWI/SNF complex components. -
PROTAC BRD9 Degrader
CFT8634 is an orally bioavailable PROTAC that targets the E3 ubiquitin ligase CRBN to degrade BRD9. This heterobifunctional molecule effectively inhibits the growth of tumor cells reliant on BRD9, making it a valuable tool for researching synovial sarcoma and SMARCB1-deficient solid tumors. CFT8634 facilitates targeted degradation through its unique binding properties, offering a strategic approach to investigate the role of BRD9 in SMARCB1-related cancers, including malignant rhabdoid tumors. -
VAV1 Molecular Glue Degrader
VAV1 degrader-3 is an orally active VAV1 molecular glue degrader with a DC50 of 7 nM. It effectively reduces immune cell activation, proliferation, and cytokine production, making it a valuable tool for studying inflammatory and autoimmune disorders. Additionally, VAV1 degrader-3 demonstrates inhibition of disease progression in experimental models such as experimental autoimmune encephalomyelitis (EAE) and collagen-induced arthritis (CIA). -
AKT PROTAC Degrader
MS15 is a selective AKT PROTAC degrader that demonstrates potent inhibition of AKT isoforms 1, 2, and 3, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively. This compound facilitates the targeted degradation of AKT, making it a valuable tool for investigating AKT-related signaling pathways. Its applications include studying cellular processes like metabolism, growth, and survival in various cancer models. -
PDE4 PROTAC Degrader
PROTAC PDE4 degrader-1 is a selective and orally active degrader targeting phosphodiesterase 4 (PDE4). It exhibits a DC50 of 41.98 μM and effectively inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. This compound demonstrates significant potential in alleviating pulmonary inflammation in LPS-induced acute lung injury models, making it a valuable tool for studying inflammatory diseases and therapeutic interventions. -
IRAK4 PROTAC Degrader
FIP22 is a potent and selective degrader of IRAK4 utilizing the PROTAC technology. It functions by inducing degradation through the formation of a ternary complex consisting of IRAK4, FIP22, and CRBN, with an EC50 of 12.63 nM. This mechanism effectively inhibits IRAK4-mediated signaling pathways, including NF-κB and MAPK pathways, making FIP22 valuable for research into conditions such as atopic dermatitis, where IRAK4 plays a critical role. -
RIPK1 PROTAC Degrader
R1-ICR-5 is a selective RIPK1 PROTAC degrader designed to mediate protein degradation via the VHL pathway. This compound promotes the degradation of RIPK1, subsequently dysregulating TNFR1 and TLR3/4 signaling pathways, enhancing the activity of NF-κB, MAPK, and IFN signaling. Additionally, R1-ICR-5 facilitates RIPK3 activation, leading to necroptosis. This reagent is applicable in research focused on triple-negative breast cancer and skin inflammation. -
PROTAC HDAC Degrader
JPS014 is a benzamide-based HDAC degrader designed to engage the Von Hippel-Lindau (VHL) E3 ligase for targeted proteolysis. It effectively degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression profiles and promoting apoptotic pathways in HCT116 cancer cells. This compound is particularly useful for studying the role of HDAC inhibition in cancer biology and elucidating mechanisms of resistance to therapies. -
PROTAC HDAC4 Degrader
PROTAC HDAC4 Degrader-1 is a selective PROTAC that targets and promotes the degradation of HDAC4, a histone deacetylase involved in regulating gene expression. This compound effectively decreases HDAC4 protein levels, leading to S phase cell cycle arrest and reduced tumor cell proliferation, as evidenced by its impact on colony formation. Additionally, PROTAC HDAC4 Degrader-1 demonstrates efficacy in vivo in H460 mouse models, making it a valuable tool for cancer research, particularly in studies related to lung cancer. -
PROTAC HDAC8 Degrader
YX862 is a selective PROTAC degrader targeting HDAC8, designed to induce robust degradation of this histone deacetylase. It achieves over 95% degradation of HDAC8 at a concentration of 250 nM in MDA-MB-231 cells. This compound serves as a valuable tool for investigating the role of HDAC8 in various biological processes and provides insights into potential therapeutic strategies for HDAC8-related diseases. -
PROTAC HDAC Degrader
JPS035 is a benzamide-derived HDAC degrader that utilizes the Von Hippel-Lindau (VHL) E3 ligase-mediated PROTAC technology. It specifically targets and degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression and promoting apoptosis in HCT116 colorectal cancer cells. This compound serves as a valuable tool for studies focused on epigenetic modulation and therapeutic strategies against HDAC-related diseases. -
ATR PROTAC Degrader
PROTAC ATR degrader-2 is a selective degrader targeting the ATR protein. It effectively induces degradation of ATR in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, demonstrating DC50 values of 22.9 nM and 34.5 nM, respectively. This compound has an IC50 of 29.6 nM against ATR, while exhibiting minimal activity against ATM and PI3K. PROTAC ATR degrader-2 promotes apoptosis, causes DNA damage, and upregulates p53 expression, thereby inhibiting cancer cell proliferation. This reagent is suitable for research applications focused on understanding mechanisms in acute myeloid leukemia. -
E3 ligase ligand-linker conjugate
Thalidomide-O-PEG2-propargyl is a synthesized E3 ligase ligand-linker conjugate that targets cereblon, a key component of the E3 ubiquitin ligase complex. This compound incorporates a two-unit PEG linker and a propargyl group, making it suitable for click chemistry applications. Thalidomide-O-PEG2-propargyl can facilitate copper-catalyzed azide-alkyne cycloaddition (CuAAc), enabling the conjugation of various azide-containing molecules, and is particularly useful in the development of targeted protein degradation strategies in chemical biology research. -
Ligands for E3 Ligase
Thalidomide-O-C8-COOH is a Thalidomide-derived ligand targeting the E3 ligase Cereblon (CRBN). This compound facilitates the recruitment of CRBN protein, serving as a vital component for the development of Proteolysis Targeting Chimeras (PROTACs). Its unique structure allows for the effective conjugation with other ligands, enabling targeted protein degradation, making it an essential tool in chemical biology and therapeutic research. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-Piperazine-PEG1-COOH serves as an E3 ligase ligand-linker conjugate, integrating a Thalidomide-derived cereblon ligand with a polyethylene glycol (PEG) linker. This compound is designed for use in PROTAC (Proteolysis Targeting Chimeras) technology, facilitating targeted protein degradation. It is suitable for research applications aimed at investigating protein regulation and therapeutic strategies in cancer and other diseases. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-PEG5-COOH is a synthesized E3 ligase ligand-linker conjugate that features a Thalidomide-derived cereblon ligand covalently attached to a polyethylene glycol (PEG) linker. This compound facilitates targeted protein degradation through the PROTAC technology by engaging the E3 ubiquitin ligase cereblon. Its primary applications include research in protein homeostasis, cancer therapeutics, and the development of new drug modalities in the field of targeted protein degradation. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-piperazine-Boc is an E3 ligase ligand-linker conjugate that serves as an intermediate in the synthesis of PROTAC targeting B-cell lymphoma 6 protein (BCL6). This compound plays a significant role in targeted protein degradation, facilitating the selective destruction of BCL6 and aiding in research related to cancer therapeutics. Its application is essential for studies focusing on E3 ligase modulation and PROTAC development in oncology. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-Propargyne-PEG2-COOH is an E3 ligase ligand-linker conjugate that combines a Thalidomide-derived cereblon ligand with a PEG-based linker suitable for PROTAC applications. This compound features an alkyne moiety, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc). It serves as a valuable tool for research in targeted protein degradation and the development of innovative therapeutic strategies. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-NH-PEG2-COOH is an E3 ligase ligand-linker conjugate that features the cereblon ligand derived from thalidomide, combined with a PEG-based linker. This compound is designed to enhance targeted protein degradation through PROTAC (Proteolysis Targeting Chimera) technology. It serves as a valuable tool for research in cellular biology and therapeutic applications by enabling precise modulation of protein levels in various biological contexts. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-O-amido-PEG-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates a cereblon ligand derived from Thalidomide. This compound is designed for use in the synthesis of PROTACs (proteolysis-targeting chimeras), facilitating targeted protein degradation in cellular systems. Its unique structure allows for selective engagement of E3 ligases, providing valuable applications in therapeutic research and drug discovery focused on the modulation of protein levels. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-O-C2-acid is an E3 ligase ligand-linker conjugate that features the Thalidomide-derived cereblon ligand, combined with a suitable linker for applications in PROTAC (Proteolysis Targeting Chimera) technology. This compound facilitates targeted protein degradation, enabling researchers to manipulate protein levels within cells. Its design supports the development of innovative therapeutic strategies by leveraging the ubiquitin-proteasome system for potential applications in cancer and other diseases. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-5-O-CH2-COOH is an E3 ligase ligand-linker conjugate that functions as a selective ligand for the Cereblon (CRBN) protein. Its primary role is to facilitate the recruitment of CRBN, making it a valuable intermediate in the synthesis of PROTAC (Proteolysis Targeting Chimeras) molecules targeting CRBN. This compound is essential for research related to targeted protein degradation and therapeutics aimed at modulating cellular proteins through ubiquitin-proteasome pathways. -
SIRT6 PROTAC Degrader
SZU-B6 is a SIRT6-protein-targeting chimeric degrader that achieves a DC50 of 45 nM and 154 nM in SK-HEP-1 and Huh-7 cell lines, respectively. It effectively inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cells. Additionally, SZU-B6 induces apoptosis and causes a cell cycle arrest in the G2/M phase in SK-HEP-1 cells, demonstrating notable antitumor efficacy in mouse models. This compound serves as a valuable tool for studying the functional roles of SIRT6 in cancer research. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-4-O-C2-NH2 hydrochloride is an E3 ligase ligand-linker conjugate featuring the cereblon ligand derived from Thalidomide. This compound is designed for use in PROTAC (proteolysis targeting chimeras) technology, facilitating the targeted degradation of specific proteins within cellular systems. Its utility in research includes studying protein turnover and exploring therapeutic strategies for various diseases through targeted protein modulation. -
PROTAC Linkers
Biotin-PEG6-Thalidomide serves as a PEG-based PROTAC linker, instrumental in the synthesis of Proteolysis Targeting Chimeras (PROTACs). This compound enhances the delivery and cellular penetration of targeted proteins for ubiquitination and subsequent degradation. Its unique design facilitates the exploration of protein modulation in various biological contexts and therapeutic applications, making it an essential tool for researchers investigating targeted protein degradation processes. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-4-O-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate utilizing the cereblon ligand derived from thalidomide. This compound plays a critical role in the assembly of PROTAC (proteolysis targeting chimera) technologies, facilitating targeted protein degradation. It is primarily used in pharmacological research to investigate E3 ligase-mediated protein modulation and to develop innovative therapeutic strategies in disease treatment. -
Ligands for E3 Ligase
Thalidomide-O-C8-Boc is a derivative of Thalidomide that functions as a ligand for the E3 ubiquitin ligase Cereblon (CRBN). This compound is utilized in the development of PROTACs by facilitating the recruitment of CRBN to target proteins through a linker. Its key biological activity involves modulating protein degradation pathways, making it valuable in drug discovery and therapeutic research targeting diseases linked to aberrant protein expressions. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-O-amido-C4-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate that incorporates a cereblon ligand derived from Thalidomide. This compound is primarily utilized in the development of PROTACs (proteolysis targeting chimeras), enabling targeted protein degradation. Its unique structure facilitates the recruitment of cognate E3 ligases, thereby promoting the efficient ubiquitination and subsequent degradation of specific target proteins, making it a valuable tool in chemical biology and therapeutic research. -
E3 Ligase Ligand-Linker Conjugates
Thalidomide-PEG4-COOH is an E3 ligase ligand-linker conjugate that combines a thalidomide-derived cereblon ligand with a PEG4 linker. This compound facilitates the targeted protein degradation through the PROTAC (Proteolysis Targeting Chimera) technology, enhancing the selective modulation of protein levels in cellular environments. It serves as a valuable tool for researchers exploring protein homeostasis, pharmacological modulation, and therapy development in various disease contexts. -
EML4-ALK PROTAC Degrader
Gly-PEG3-BA is an EML4-ALK PROTAC degrader that targets the EML4-ALK fusion protein. This compound exhibits a DC50 of 0.50 μM for EML4-ALK in H3122 cells and a DC50 of 20.15 μM for EGFR mutant (L858R/T790M) levels in H1975 cells. Gly-PEG3-BA demonstrates notable antiproliferative effects, with IC50 values of 0.84 μM against H3122 cells and 20.74 μM against H1975 cells. It is a valuable tool for research in non-small cell lung cancer. -
EML4-ALK/EGFR PROTAC Degrader
Lys-PEG3-BA is a novel EML4-ALK/EGFR PROTAC degrader that influences target proteins through the ubiquitin-proteasome pathway. With DC50 values of 1.32 μM against H3122 (EML4-ALK) cells and 19.66 μM for H1975 (EGFR-L858R/T790M) cells, it effectively inhibits cell proliferation. This compound serves as a valuable tool for research into non-small cell lung cancer and the mechanisms underlying targeted protein degradation. -
EGFR PROTAC Degrader
PROTAC EGFR degrader 17 is a potent EGFR-targeted PROTAC degrader with a DC50 value of 0.49 nM. This reagent facilitates the ubiquitination and subsequent degradation of the epidermal growth factor receptor (EGFR). It is particularly useful for research applications related to various forms of cancer, including non-small cell lung cancer, providing a valuable tool for investigating targeted degradation pathways in oncogenesis. -
EGFR PROTAC Degrader
PROTAC EGFR degrader 12 is a PROTAC designed to selectively target and degrade mutant forms of epidermal growth factor receptor (EGFR). It demonstrates potent biological activity with IC50 values under 50 nM against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells). This reagent is valuable for research applications focused on understanding and treating EGFR-driven cancers, particularly those with resistant mutations. -
EGFR PROTAC Degrader
PROTAC EGFR degrader 16 is a selective degrader designed to target the epidermal growth factor receptor (EGFR). It exhibits DC50 values of less than 50 nM in various cell lines, including NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R), and NCI-H1976 + CS (EGFR L858R-T970M-L797S). This compound is valuable for investigating EGFR-driven cancers, particularly non-small cell lung cancer, facilitating research into targeted degradation therapies. -
EGFR PROTAC Degrader
PROTAC EGFR Degrader 10 is an advanced PROTAC agent targeting the epidermal growth factor receptor (EGFR) with a DC50 of less than 100 nM. It effectively binds to CRBN-DDB1 with a Ki of 37 nM, facilitating the degradation of EGFR as well as focal adhesion kinase (FAK) and RSK1. This compound demonstrates potent inhibitory effects on the proliferation of BaF3 cells, including those with EGFR mutations, with an IC50 of less than 150 nM. PROTAC EGFR Degrader 10 is suitable for studies focused on targeted protein degradation and cancer research. -
EGFR PROTAC Degrader
PROTAC EGFR Degrader 11 is a targeted degrader specifically designed to modulate the epidermal growth factor receptor (EGFR) through the PROTAC mechanism. It effectively binds to the CRBN-DDB1 complex with a Ki value of 36 nM and has a DC50 of less than 100 nM for EGFR degradation. This compound demonstrates significant biological activity by degrading not only EGFR but also focal adhesion kinase (FAK) and RSK1. Additionally, it inhibits the proliferation of BaF3 cells with both wild-type and mutant EGFR variants, achieving an IC50 of less than 100 nM, making it a valuable tool for cancer research focused on EGFR-related pathways.
