Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC p300/CBP Degrader
dCBP-1 is a potent and selective heterobifunctional PROTAC degrader of p300/CBP, utilizing a cereblon ligand for E3 ligase recruitment. It effectively eliminates oncogenic enhancer activity driving MYC expression and demonstrates strong cytotoxicity against multiple myeloma cells, making it a valuable tool for epigenetic and cancer research. -
androgen receptor (AR) PROTAC degrader
BMS-986365 (CC-94676) is an orally active, selective PROTAC degrader targeting the androgen receptor (AR), including AR mutants. It functions via cereblon (CRBN)-mediated ubiquitination and proteasomal degradation of AR. BMS-986365 exhibits strong in vivo efficacy by suppressing AR signaling and inhibiting tumor growth in advanced prostate cancer models, making it a promising candidate for therapeutic development. -
PROTAC IRAK4 degrader
KT-474 (SAR444656) is a selective small-molecule PROTAC degrader of IRAK4, under development for the treatment of TLR/IL-1R–mediated autoimmune diseases. It effectively suppresses R848 (TLR7/8)- and LPS-induced IL-6 and IL-8 production in peripheral blood mononuclear cells (PBMCs), highlighting its potential as an anti-inflammatory therapeutic. -
PROTAC STAT3 Degrader
SD-36 is a selective PROTAC degrader of STAT3 that induces potent degradation of STAT3 protein both in vitro and in vivo, with minimal impact on other STAT family members. By suppressing STAT3-driven transcriptional programs, SD-36 inhibits the proliferation of acute myeloid leukemia and anaplastic large-cell lymphoma cells through cell cycle arrest and apoptosis. In xenograft mouse models, SD-36 achieves complete and sustained tumor regression at well-tolerated doses, making it a promising tool for cancer research and targeted therapy development. -
PROTAC BRD4 Degrader
GNE-987 is a highly potent PROTAC degrader of BRD4, composed of a BET inhibitor, a von Hippel-Lindau (VHL) ligand, and a ten-methylene linker. It binds both BD1 and BD2 bromodomains of BRD4 with low nanomolar affinity (IC₅₀ = 4.7 and 4.4 nM) and induces BRD4 degradation with a DC₅₀ of 0.03 nM in EOL-1 AML cells. GNE-987 is also suitable for use in PROTAC–Antibody Conjugates (PAC), making it a valuable tool for targeted protein degradation and epigenetic cancer research. -
PROTAC EP300 Degrader
JQAD1 is a CRBN-dependent PROTAC selectively targeting EP300 for degradation. It effectively reduces EP300 protein levels and H3K27ac histone acetylation, resulting in apoptosis. JQAD1 is a valuable tool for investigating EP300 function and epigenetic regulation in cellular processes. -
BTK Inhibitor
Zelebrudomide (NX-2127) is a novel, potent BTK degrader that induces proteasomal degradation through targeted ubiquitination, rather than direct inhibition. In addition to degrading BTK, Zelebrudomide (NX-2127) enhances immune responses by stimulating T cell activation and increasing IL-2 production in primary human T cells, supporting its potential in cancer and immunotherapy research.
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PROTAC CDK2/9 Degrader
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual PROTAC degrader targeting CDK2 (DC₅₀ = 62 nM) and CDK9 (DC₅₀ = 33 nM), constructed by linking a CDK inhibitor to a cereblon ligand. It effectively inhibits PC-3 prostate cancer cell proliferation (IC₅₀ = 0.12 µM) by inducing cell cycle arrest in the S and G2/M phases, making it a valuable tool for cancer and cell cycle research. -
WDR5 Degrader
MS67 is a highly potent and selective PROTAC degrader of WD40 repeat domain protein 5 (WDR5), exhibiting minimal activity against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. Its strong anticancer activity highlights its utility as a targeted tool for studying WDR5-related epigenetic regulation and cancer therapy. -
PROTAC SGK3 degrader
SGK3-PROTAC1 is a PROTAC molecule designed to selectively degrade SGK3 by linking the 308-R SGK inhibitor to the VHL-binding ligand VH032. Through recruitment of the VHL E3 ligase, SGK3-PROTAC1 induces proteasomal degradation of SGK3, providing a targeted approach for studying SGK3 function in cellular signaling and disease. -
PROTAC SMARCA2/SMARCA4 degrader
AU-15330 is a PROTAC degrader targeting the SWI/SNF chromatin remodeling ATPase subunits SMARCA2 and SMARCA4. It effectively suppresses tumor growth in prostate cancer xenograft models and enhances the therapeutic efficacy of the AR antagonist enzalutamide. AU-15330 also induces remission in castration-resistant prostate cancer models, demonstrating strong antitumor activity with a favorable safety profile. -
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. -
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. -
Her3 PROTAC Degrader
PROTAC Her3 Degrader-8 is a potent Her3 PROTAC degrader that facilitates the ubiquitination and subsequent degradation of the Her3 protein. This compound is particularly relevant for studies focused on lung adenocarcinoma and ovarian cancer, enabling researchers to investigate the role of Her3 in these malignancies. The design incorporates a specific Her3 ligand, an E3 ligase ligand, and a linker, which optimizes its efficacy as a targeted degradation tool in research applications. -
EGFR PROTAC Degrader
SJF-1528 is a potent EGFR PROTAC degrader that selectively targets wild-type EGFR and Exon 20 Ins mutant EGFR, exhibiting DC50 values of 39.2 nM and 736.2 nM, respectively, in OVCAR8 and HeLa cells. This compound facilitates the ubiquitination and subsequent degradation of EGFR and also affects HER2 levels. SJF-1528 is valuable for breast cancer research, providing insights into targeted degradation mechanisms and alterations in growth factor signaling pathways. -
PARP PROTAC Degrader
PROTAC PARP1 degrader-2 is a targeted protein degradation compound designed to specifically degrade PARP1. With a DC50 of less than 10 nM in MDA-MB-231 cells, it demonstrates potent efficacy in inducing degradation. Additionally, this compound inhibits cell viability in MDA-MB-436 cells with an IC50 of less than 100 nM, making it a valuable tool for research in cancer therapeutics and the mechanistic study of PARP1 function. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-44 is a selective degrader targeting the EZH2-PRC2 complex through the recruitment of the CRBN E3 ligase, facilitating proteasome-mediated degradation of EZH2, SUZ12, and EED. This process leads to a marked reduction in H3K27me3 and CARM1 levels, resulting in potent antiproliferative effects. It induces mitochondrial dysfunction and promotes apoptosis by modulating Bcl-2 family proteins, demonstrating minimal cytotoxicity in normal human mammary epithelial, liver, and kidney cells. PROTAC EZH2 Degrader-44 serves as an effective research tool for investigating targeted therapies in triple-negative breast cancer. -
PARP14 PROTAC Degrader
RBN012811 is a selective PROTAC degrader that targets PARP14, facilitating its degradation through a ternary complex with cereblon by binding at the NAD+ site. With an IC50 of 10 nM, RBN012811 efficiently reduces endogenous PARP14 levels in various cell lines and primary human macrophages. This reduction is associated with decreased IL-10 production and IFN-β mRNA, alongside an increase in phosphorylated STAT1, thereby enhancing inflammatory signaling and inhibiting interferon-induced ADPr condensate formation. RBN012811 also influences viral replication dynamics, promoting HSV1 replication while diminishing VSV replication, making it valuable for research in cancer biology and viral infections. -
KAT2A/KAT2B PROTAC Degrader
PROTAC KAT2A/B degrader-1 is a targeted degrader that selectively induces the degradation of histone acetyltransferases KAT2A and KAT2B. This compound demonstrates significant inhibition of proliferation in acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 is a valuable tool for studying the roles of KAT2A and KAT2B in cancer biology and may facilitate the development of novel therapeutic strategies for these malignancies. -
Molecular Glue
MNN-02-155 is a bivalent molecular glue that binds simultaneously to p300/CBP and BCL6. This compound effectively activates the BCL6-target reporter gene, leading to significant induction of cell death. MNN-02-155 is particularly relevant for research into diffuse large B cell lymphomas (DLBCLs), providing insights into potential therapeutic strategies involving BCL6 modulation.
