Catalog No.
Product Name
Application
Product Information
Citations
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AKT PROTAC Degrader
MS21 is a potent AKT PROTAC degrader designed to selectively target and degrade AKT proteins. This compound effectively inhibits mutations within the PI3K/PTEN pathway, leading to suppressed tumor cell proliferation and induction of cell cycle arrest. MS21 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development. -
EGFR PROTAC Degrader
HJM-561 is a selective EGFR PROTAC degrader that effectively targets and degrades EGFR mutations resistant to conventional therapies, such as Osimertinib. It demonstrates potent degradation activity against key triple mutations including Del19/T790M/C797S (DC50: 9.2 nM) and L858R/T790M/C797S (DC50: 5.8 nM). HJM-561's mechanism provides promising potential for anti-tumor applications in the treatment of EGFR-driven malignancies. -
FKBP12F36V PROTAC Degrader
dTAGV-1 hydrochloride is a highly selective degrader targeting FKBP12F36V-tagged proteins through the PROTAC mechanism. This compound effectively induces the degradation of FKBP12F36V-Nluc in vivo, making it a valuable tool for studies involving targeted protein degradation. Its application in research facilitates the investigation of protein function, dynamics, and the development of therapies that exploit the proteolysis pathway. -
GPX4 PROTAC Degrader
PROTAC GPX4 degrader-1 functions as a targeted protein degradation agent specifically for GPX4. It exhibits a DC50 of 0.03 μM in HT1080 cells, demonstrating potent activity in promoting the degradation of GPX4. This compound is applicable in research exploring the role of GPX4 in various cellular processes and the therapeutic potentials of targeting antioxidant defenses in disease models. -
RAF PROTAC Degrader
SJF-0628 is a RAF PROTAC degrader that facilitates the targeted degradation of BRAF protein in cancer cell lines, specifically in colorectal cancer models (Colo-205, LS-411N, HT-29, RKO) and the triple-negative breast cancer line DU-4475. This compound significantly reduces levels of phosphorylated MEK and ERK in DU-4475 cells, demonstrating notable anti-tumor activity. SJF-0628 is valuable for research studies focused on the mechanisms of colorectal cancer and triple-negative breast cancer. -
PROTAC Degrader
HDAC6 degrader-1 is a PROTAC degrader targeting HDAC6, exhibiting a DC50 value of 3.8 nM in MM.1S cells. This compound efficiently induces the degradation of HDAC6 through a bifunctional strategy, linking a ligand for the E3 ligase Pomalidomide with a ligand for the target protein Nexturastat A via a specialized linker. Its application is vital for investigating the role of HDAC6 in cellular processes and potential therapeutic effects in various diseases. -
EZH2 Degrader
NUCC-0226272 is a potent PROTAC that facilitates the targeted degradation of EZH2. This compound exhibits significant anti-proliferative effects, making it a valuable tool for investigating the role of EZH2 in cancer biology. Its application in cancer research provides insights into potential therapeutic strategies for malignancies associated with EZH2 dysregulation. -
SMARCA2 PROTAC Degrader
YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 and H1975 cell lines, respectively. This reagent induces the degradation of SMARCA2, exhibiting synthetic lethality towards SMARCA4-deficient cells and selectively inhibiting growth in SMARCA4 mutant lung cancer cells. YD23 also reduces chromatin accessibility in SMARCA4 deficient cells, impacting genes associated with cell cycle and growth regulation. It is a valuable tool for researching non-small cell lung cancer (NSCLC) and evaluating tumor growth in SMARCA4-mutant xenograft models. -
PROTAC FKBP12 Degrader
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader designed to facilitate targeted protein degradation. It achieves this by covalently modifying DCAF16, an E3 ligase, thereby enhancing the stability of FKBP12 degradation within biological systems. The compound consists of a molecular glue linking the ubiquitin E3 ligase ligand KB02 with SLF, enabling efficient degradation of FKBP12 for various research applications in protein regulation and degradation pathways. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-8 is a proteolysis-targeting chimera (PROTAC) that engages both von Hippel-Lindau (VHL) and BRD4, exhibiting IC50 values of 1.1 nM for BRD4 BD1 and 1.4 nM for BRD4 BD2. This compound effectively promotes the degradation of BRD4 protein in PC3 prostate cancer cells, making it a valuable tool for research into BRD4-related signaling pathways and cancer therapeutics. Its high potency highlights its potential use in studying mechanisms of protein regulation and developing novel cancer treatments. -
PROTAC BRD Degrader
β-NF-JQ1 is a PROTAC that targets bromodomain-containing (BRD) proteins by leveraging β-NF as a ligand for the Aryl Hydrocarbon Receptor (AhR) E3 ligase. This compound facilitates the degradation of BRD proteins through the recruitment of AhR, leading to effective protein knockdown. β-NF-JQ1 demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology and the development of targeted therapeutic strategies. -
CBP/p300 PROTAC Degrader
CBPD-268 is a highly potent CBP/p300 PROTAC degrader, exhibiting a DC50 value of ≤ 0.03 nM. This compound effectively induces degradation of CBP/p300 and demonstrates significant inhibition of cell growth, showcasing its antitumor potential. CBPD-268 is particularly relevant for research into androgen receptor-positive prostate cancer, facilitating studies on novel therapeutic strategies. -
FKBP12(F36V) Inhibitor
dTAGV-1-NEG is a diastereomer that acts as a heterobifunctional negative control for dTAGV-1, specifically targeted at FKBP12(F36V). This compound is utilized in research to study the selectivity and efficacy of FKBP12(F36V) degraders, helping to elucidate cellular mechanisms and pathways influenced by FKBP12 modulation. Its role as a control reagent makes it essential for validating experimental results in protein degradation studies. -
Isoform of SHP2-D26
SHP2-D26 isomer-1 is an isoform of the SHP2-D26 degrader, designed specifically for targeted protein degradation applications. This compound does not induce degradation of SHP2 at concentrations ranging from 3 to 1000 nM. As a component of PROTAC technology, SHP2-D26 isomer-1 serves as a valuable tool for studying SHP2's role in signaling pathways and assessing the therapeutic potential of SHP2 modulation in various diseases. -
PROTAC Degrader
SNX7886 is a potent PROTAC degrader targeting CDK8 and CDK19. It effectively induces degradation of CDK8 and CDK19, achieving up to 90% and 80% degradation, respectively, in 293 cells. This compound is valuable for research applications in understanding the role of CDK8/19 in various biological processes and cancer pathways. -
TBK1 Degrader
PROTAC TBK1 Degrader-2 is a targeted protein degrader designed to selectively degrade the serine/threonine kinase TANK-binding kinase 1 (TBK1) with a DC50 of 15 nM and Kd of 4.6 nM, exhibiting a maximum efficiency of 96%. Additionally, this compound also influences IkB kinase IKKε, demonstrating an IC50 of 8.7 nM, and displays a low selectivity over TBK1 with an IC50 of 1.3 nM. This reagent is suitable for investigating TBK1-related signaling pathways and potential therapeutic applications in various diseases. -
EZH2 PROTAC Degrader
MS8847 is a powerful EZH2 PROTAC degrader that utilizes the E3 ligase von Hippel-Lindau (VHL) to promote the degradation of EZH2 through the ubiquitin-proteasome system. This compound demonstrates robust anti-proliferative effects in acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cell lines. MS8847 serves as a valuable tool for investigating the role of EZH2 in oncogenic signaling pathways and developing targeted therapies for EZH2-dependent malignancies. -
PROTAC CSK Degrader
DB-3-291 is a potent and selective PROTAC degrader targeting the protein CSK, exhibiting a Kd of 1 nM. This compound facilitates the degradation of CSK through its specific interaction with the E3 ligase, enabling in-depth studies of CSK-related biological pathways and providing insights into potential therapeutic strategies. It is valuable for researchers investigating targeted protein degradation and cancer biology. -
PROTAC KRAS G12C Degrader
PROTAC KRAS G12C degrader-1 is a Cereblon-based PROTAC targeting the KRAS G12C mutant. This compound promotes the formation of a dimer between Cereblon and KRAS G12C, leading to the degradation of GFP-tagged KRAS G12C in reporter cell systems. It serves as a valuable tool for research on targeted degradation strategies in KRAS-driven cancers. -
PROTAC CRBN Degrader
TD-165 is a PROTAC (proteolysis-targeting chimera) that targets cereblon (CRBN) for selective degradation of proteins. This compound features a CRBN ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group, facilitating targeted ubiquitination and proteolytic degradation of specific proteins involved in cellular processes. TD-165 is suitable for research applications focused on targeted protein degradation, therapeutic development, and elucidating protein function in various biological contexts. -
PROTAC PARP1 Degrader
PROTAC PARP1 Degrader functions as a targeted protein degradation agent that specifically targets PARP1 through the MDM2 E3 ligase. This compound effectively induces PARP1 cleavage and promotes apoptosis in cancer cells, making it valuable for research in cancer therapies. The structure includes the MDM2 ligand, the PARP1 ligand, and a PEG-based linker, facilitating efficient delivery and degradation of the target protein. -
PROTACs
PROTAC BRD9 Degrader-4 is a bifunctional degrader targeting BRD9 through the proteolysis-targeting chimera (PROTAC) mechanism. It effectively induces degradation of BRD9, thereby altering oncogenic pathways associated with various cancers. This compound is utilized in cancer research to study the therapeutic potential of BRD9 modulation and the implications of targeted degradation in tumor biology. -
BRD42/BRD4 Degrader
IBG1 is a molecular glue degrader that selectively targets BRD2 and BRD4, exhibiting a degradation capability with a DC50 of 0.15 nM. Notably, IBG1 does not significantly impact the paralogue BRD3. This compound effectively inhibits the growth of cancer cells and is a valuable tool for research focused on tumor biology and therapeutic strategies. -
PROTAC IRAK Degrader
Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses. -
MET Degrader
PRO-6E is a PROTAC that targets Cereblon to induce degradation of the MET protein. It achieves up to 81.9% degradation of MET at 1 μM in MKN-45 cells, effectively inhibiting tumor growth both in vitro and in vivo. Additionally, PRO-6E promotes apoptosis and cell cycle arrest, making it a valuable tool for research on MET-related oncogenic processes. -
Kinases PROTAC
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions. -
dTAG-13 Negative Control
dTAG-13-NEG serves as a negative control for dTAG-13, a PROTAC-based bifunctional degrader that selectively targets FKBP12F36V in the presence of a protein of interest. While dTAG-13 promotes the degradation of FKBP12F36V, dTAG-13-NEG allows for the assessment of specificity and background in experimental setups involving this pathway. This compound is essential for validating experimental results when studying protein degradation mechanisms and their implications in cellular biology. -
SMARCA2 PROTAC degrader
SMD-3040 is a selective SMARCA2 PROTAC degrader with a DC50 of 12 nM and a maximal degradation efficiency of 91%. This compound effectively inhibits tumor cell proliferation, demonstrating significant antitumor activity. SMD-3040 is particularly useful in studies related to various tumors, including melanoma. -
PROTAC BRD4 Degrader
PROTAC BET Degrader-10 is a selective degrader targeting the BET protein BRD4 through a PROTAC mechanism, featuring a DC50 of 49 nM. This compound utilizes ligands for Cereblon and BRD4, promoting the ubiquitination and subsequent degradation of BRD4. It serves as a valuable tool for investigating the role of BRD4 in various biological processes and cancer-related research applications. -
PROTAC BTK Degrader
NRX-0492 is an orally active PROTAC BTK degrader that promotes the ubiquitination and proteasomal degradation of Bruton's tyrosine kinase (BTK) with DC50 values as low as 0.2 nM. This compound effectively inhibits B cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion, demonstrating significant antitumor activity against chronic lymphocytic leukemia. NRX-0492 comprises a BTK inhibitor, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, making it a valuable tool for studying BTK-related pathways and therapies. -
RNA RIBOTAC Degrader
Dovitinib-RIBOTAC TFA is a targeted RNA RIBOTAC degrader that specifically binds to and degrades pre-miR-21. This compound demonstrates significant anti-tumor activity and effectively inhibits breast cancer metastasis. It serves as a valuable tool for research involving RNA-targeted degradation and its implications in cancer biology. -
IRAK4 Degrader
KTX-951 is a selective IRAK4 degrader that employs a PROTAC mechanism to facilitate targeted degradation of IRAK4 and IMiD substrates, including Ikaros and Aiolos. With a Kd of 3.5 nM and DC50 values of 13 nM for IRAK4, Ikaros, and Aiolos, KTX-951 demonstrates potent biological activity. It also exhibits an IC50 of 35 nM against OCl-Ly10 CTG, indicating its potential use in antitumor research applications. -
JAK1 PROTAC Degrader
PROTAC JAK1 Degrader 1 is a selective PROTAC agent targeting JAK1, exhibiting a DC50 of 214 nM. This compound initiates rapid degradation of JAK1, leading to significant antitumor activity. It serves as a valuable tool for investigating JAK1-related signaling pathways and developing therapeutic strategies for malignancies driven by JAK1 dysregulation. -
PROTAC FKBP Degrader
PROTAC FKBP Degrader-3 is a proteolysis-targeting chimera that utilizes a FKBP ligand binding group and a von Hippel-Lindau (VHL) E3 ligase recruiting moiety linked by a flexible linker. This compound effectively induces the degradation of FKBP12, demonstrating potent biological activity in targeted protein degradation. It is primarily used in research applications related to protein homeostasis, cellular signaling mechanisms, and therapeutic development strategies for modulating protein levels. -
EGFR Degrader
MS154 is a novel E3 ligase cereblon-recruited degrader specifically targeting epidermal growth factor receptor (EGFR). It has demonstrated potent degradation of the EGFR L858R mutant in cancer cell lines with Kd values of 1.8 nM and 3.8 nM for wild-type and mutant EGFR, respectively. This selective degradation mechanism highlights its potential as an anticancer agent, particularly in lung cancer treatment. MS154 operates through an E3 ligase-dependent pathway, representing a promising therapeutic strategy for treating EGFR-driven malignancies. -
PROTAC RIPK degrader
PROTAC RIPK degrader-6 is a Cereblon-based protein-targeting chimeric molecule designed for the degradation of RIP Kinase. This compound employs a RIP2 kinase inhibitor linked through a suitable spacer to a cereblon ligand, facilitating targeted proteolysis of RIPK. Prominent applications include investigations into kinase-related signaling pathways and the development of innovative therapeutic strategies for diseases associated with RIPK dysregulation. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-1 is a novel PROTAC that utilizes ligands for both Cereblon and BRD4, exhibiting an IC50 of 41.8 nM against the BRD4 bromodomain 1 (BD1). This compound promotes the degradation of BRD4 protein, leading to a significant decrease in c-Myc expression. It is designed for research applications aimed at understanding the role of BRD4 in transcriptional regulation and its implications in various cancers. -
PROTAC ERRα Degrader
PROTAC ERRα Degrader-3 is a selective degrader targeting estrogen-related receptor alpha (ERRα) through a von Hippel-Lindau-based mechanism. This compound effectively induces the degradation of ERRα protein by over 80% at a concentration of 30 nM, while showing no activity against ERRβ and ERRγ. It serves as a valuable tool for researchers investigating the role of ERRα in various biological processes and disease states. -
VEGFR-2 Inhibitor
VEGFR-2-IN-39 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), with an IC50 of 208.6 nM. This compound effectively inhibits the proliferation of EA.hy926 cells, a human umbilical vein endothelial cell line, in a concentration-dependent manner, exhibiting an IC50 of 38.65 µM. VEGFR-2-IN-39 has low toxicity, making it suitable for further research applications in angiogenesis and vascular biology. -
PROTAC EED Degrader
PROTAC EED Degrader-2 is a von Hippel-Lindau-based PROTAC that selectively targets the embryonic ectoderm development (EED) subunit of the polycomb repressive complex 2 (PRC2), exhibiting a pKD of 9.27. This compound acts as an effective inhibitor, demonstrating a pIC50 of 8.11, facilitating the degradation of EED and providing valuable insights for research on PRC2-related epigenetic regulation and its implications in various biological processes. Applications include studies on gene expression regulation and potential therapeutic targets in cancer and developmental biology. -
PROTAC IDO1 Degrader
PROTAC IDO1 Degrader-1 is a novel compound targeting indoleamine 2,3-dioxygenase 1 (IDO1) through the engagement of Cereblon E3 ligase, facilitating its ubiquitination and subsequent degradation. With a reported DC50 of 2.84 μM, this degrader enhances the anti-tumor efficacy of HER2 CAR-T cells, making it a valuable tool for research in cancer immunotherapy and targeted degradation methods. Its ability to modulate IDO1 levels opens avenues for investigations into metabolic regulation and tumor microenvironment interactions. -
PROTAC AR Degrader
ARD-69 is a PROTAC degrader that targets the androgen receptor (AR) through the E3 ubiquitin ligase VHL, facilitating AR protein degradation in AR-positive prostate cancer cells. By binding to both the AR ligand-binding domain and VHL, ARD-69 promotes the recruitment of AR to the E3 ubiquitin ligase complex, leading to proteasomal degradation and subsequent inhibition of AR signaling pathways, including AR-regulated gene expression such as PSA and TMPRSS2. ARD-69 is a valuable tool for studying mechanisms underlying castration-resistant prostate cancer (mCRPC). The compound consists of an AR antagonist, a specific PROTAC linker, and a VHL-type E3 ubiquitinase ligand. -
PROTAC BRD4 Degrader
KB02-JQ1 is a selective PROTAC BRD4 degrader that functions as a molecular glue, specifically targeting BRD4 while sparing BRD2 and BRD3. This compound induces BRD4 degradation by covalently modifying the E3 ligase DCAF16, thereby enhancing the stability and duration of protein degradation in biological systems. Its unique design, which incorporates JQ1 linked to the ubiquitin E3 ligase ligand KB02, facilitates targeted modulation of gene expression, making it a valuable tool for research in cancer biology and therapeutic development. -
TYK2 Degrader
PROTAC TYK2 degradation agent1 is a selective degrader targeting TYK2, effectively facilitating its degradation with a DC50 value of 14 nM. This compound highlights significant biological activity in modulating TYK2 levels, making it a useful tool for investigating autoimmune diseases. Research applications include studying the role of TYK2 in inflammatory pathways and evaluating potential therapeutic strategies. -
PROTAC CDK4/6 Degrader
BSJ-02-162 is a potent PROTAC degrader targeting CDK4/6 through the utilization of a thalidomide-based E3 ligase ligand and a selective CDK4/6 inhibitor. This compound effectively recruits ubiquitin ligases to facilitate the targeted degradation of CDK4/6, thereby modulating cellular responses to cell cycle regulation. BSJ-02-162 is designed for research applications exploring cancer therapies and the mechanisms of protein homeostasis within tumor cells. -
PTPN2 Degrader
PROTAC PTPN2 degrader-1 is an effective degrader of the protein tyrosine phosphatase PTPN2. This compound facilitates target protein degradation through the proteasome pathway, enabling the modulation of cellular signaling related to cancer and metabolic diseases. Its application in research may provide insights into the therapeutic potential of targeting PTPN2 in various disease contexts. -
CDK2 molecular glue Degrader
CDK2 degrader 1 is a selective molecular glue degrader targeting cyclin-dependent kinase 2 (CDK2). It effectively induces ubiquitination and proteasomal degradation of CDK2 by binding to cereblon, achieving a Dmax greater than 80% and a Ki greater than 1 μM. This compound is utilized in cancer research, providing insights into tumor biology and potential therapeutic strategies. -
PROTAC EED Degrader
PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC that selectively targets EED with a pKD of 9.02. This compound functions as a polycomb repressive complex 2 (PRC2) inhibitor, exhibiting an inhibitory potency characterized by a pIC50 of 8.17. It serves as a valuable tool for researching the modulation of PRC2 activity and its implications in cancer biology and epigenetic regulation. -
IKZF2/CK1α Molecular Gel
DEG-77 is a molecular glue that targets IKZF2 and CK1α, demonstrating DC50 values of 15.3 nM and 10 nM, respectively. This compound exerts notable anti-tumor effects by enhancing the transcription of the pro-apoptotic protein Bax and promoting the expression of the cell cycle regulator p21. DEG-77 is relevant for research in acute myeloid leukemia (AML), diffuse large B-cell lymphoma, and ovarian cancer. -
RIPK1 PROTAC Degrader
LD4172 is a selective RIPK1 PROTAC degrader that exhibits a Ki of 4.8 nM. It facilitates RIPK1 protein degradation through the formation of a ternary complex with RIPK1 and VHL E3 ligase, leading to ubiquitination and proteasomal degradation. LD4172 effectively inhibits TNF-induced classical NF-κB signaling in TRAF2-deficient cells, significantly reducing IκBα phosphorylation and IL-8 production. Additionally, it promotes apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy, making it a valuable chemical probe for studying RIPK1-related functions in melanoma and colon cancer research.
