Catalog No.
Product Name
Application
Product Information
Citations
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CRBN degrader
Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3. -
PDE6D/IKZF1/IKZF3/CK1α Degrader
FPFT-2216 is a “molecular glue” degrader that facilitates the proteasomal degradation of multiple target proteins, including phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), as well as casein kinase 1α (CK1α). By promoting selective ubiquitination through E3 ligase recruitment, FPFT-2216 modulates key regulatory pathways and holds promise for research in oncology and inflammatory diseases. -
PROTAC CRBN Degrader
CRBN-6-5-5-VHL is a potent and selective VHL-based PROTAC degrader targeting cereblon (CRBN), with a DC₅₀ of 1.5 nM. It selectively degrades CRBN without affecting neo-substrates IKZF1 and IKZF3. -
PROTAC CDK4/6 Degrader
BSJ-03-204 triTFA is a potent and selective PROTAC degrader targeting CDK4/6, constructed using ligands for cereblon and CDK. Based on Palbociclib, it exhibits IC₅₀ values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and shows anti-cancer activity, making it a valuable tool for cell cycle and oncology 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. -
IKAROS Protein Degrader
MGD-28 is a potent IKAROS protein degrader that functions through Cereblon (CRBN)-dependent mechanisms. It effectively degrades IKZF1 (DC50=3.8 nM), IKZF2 (DC50=56.3 nM), and IKZF3 (DC50=7.1 nM), along with CK1α (DC50=7.8 nM), in a dose-dependent manner. MGD-28 exhibits significant antiproliferative activity, making it a valuable tool for research in multiple myeloma and related hematological malignancies. -
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. -
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. -
Stable Isotope
Lenalidomide-d5 is a stable isotope-labeled derivative of Lenalidomide, an immunomodulatory compound that functions as a molecular glue. By acting as a ligand for the ubiquitin E3 ligase cereblon (CRBN), it facilitates the selective ubiquitination and subsequent degradation of the transcription factors IKZF1 and IKZF3. Lenalidomide-d5 is pivotal for research in cancer biology, particularly for investigating the mechanisms of action in mature B-cell lymphomas, including multiple myeloma, and for studying its effects on cytokine release from T cells. -
GCK/MAP4K2 Inhibitor
TL4-12 is a selective inhibitor of MAP4K2 and GCK, demonstrating a dose-dependent ability to downregulate IKZF1 and BCL-6. This compound effectively inhibits cell proliferation in multiple myeloma with an IC50 of 37 nM, and it also induces apoptosis in cancerous cells. TL4-12 holds potential for overcoming resistance to immunomodulatory agents in the treatment of multiple myeloma. -
Stable Isotope
Lenalidomide-d4 is a deuterium-labeled derivative of Lenalidomide, functioning as a stable isotope for advanced chemical research. As an orally active immunomodulator, Lenalidomide targets the cereblon (CRBN) ubiquitin E3 ligase, leading to the selective ubiquitination and degradation of transcription factors IKZF1 and IKZF3. This activity is particularly relevant in the context of mature B-cell lymphomas, including multiple myeloma, where Lenalidomide-d4 has been shown to inhibit tumor growth and promote IL-2 release from T cells. This reagent is suitable for studies in drug mechanisms and development within the field of oncology. -
CRBN Modulator
AG6033 is a novel modulator of the cereblon (CRBN) protein. This compound effectively suppresses various tumor cell lines by influencing the interactions between CRBN and key antitumor target proteins, leading to the degradation of GSPT1 and IKZF1. AG6033 has demonstrated a CRBN-dependent cytotoxic effect, making it a valuable tool for research in cancer biology and the development of targeted therapies. -
Triple IKZF1/2/3 Degrader
MGD-22 is a molecular glue and an orally active degrader of the IKZF1/2/3 proteins, with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. This compound exhibits significant anti-proliferative effects on various hematological cancer cell lines and induces apoptosis in these cells. Additionally, MGD-22 demonstrates robust anti-tumor efficacy in mouse models with NCI-H929 or WSU-DLCL-2 xenografts. It is a valuable tool for investigating hematological malignancies, particularly multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL). -
Ikaros/Helios Degrader
ALV1 is a molecular glue degrader targeting Ikaros (IKZF1) and Helios (IKZF2), with degradation constants (DC50) of 2.5 nM and 10.3 nM, respectively. It interacts with cereblon (CRBN) with an IC50 of 0.55 μM, promoting CRBN-Helios dimerization. ALV1 is useful for investigating the roles and mechanisms of regulatory T cells in various biological contexts. -
BTK/IKZF1/3 PROTAC Ligand
BTK/IKZF1/3 ligand 1 is a PROTAC ligand targeting Bruton's tyrosine kinase (BTK) and the Ikaros family zinc finger proteins (IKZF1/3). This compound can be conjugated with E3 ligase ligands and linkers to produce PROTAC BTK/IKZF1/3 Degrader-1, facilitating targeted protein degradation. It is valuable for cancer research, supporting investigations into therapeutic strategies aimed at modulating BTK and IKZF1/3 activity in malignant cells. -
BTK/IKZF1/3 PROTAC Degrader
PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally bioavailable degrader targeting BTK, IKZF1, and IKZF3 through the PROTAC mechanism. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research, particularly in the context of lymphoma. Its unique mechanism of action allows for the targeted degradation of specific oncogenic proteins, facilitating studies in therapeutic strategies and disease mechanisms. -
Multiple Target PROTAC
GT19630 is a multiple target PROTAC designed to degrade c-MYC, CK1α, GSPT1, and IKZF1/2/3 proteins. This compound effectively targets and reduces the levels of these proteins in various tumor cell lines, making it a valuable tool for studying diseases characterized by high c-MYC expression, including cancer, cardiovascular disorders, cerebrovascular diseases, and viral infections. Researchers can utilize GT19630 to further investigate the therapeutic potential of protein degradation in relevant biological contexts. -
IKZF2/CK1α Molecule Glue
DEG-35 is a CRBN-dependent dual degrader targeting IKZF2 and CK1α, exhibiting DC50 values of 1.4 nM and 4.4 nM, respectively. This compound activates the p53 apoptosis pathway, highlighting its potential in promoting cell death. DEG-35 serves as a valuable tool for research focused on Acute Myeloid Leukemia (AML), providing insights into targeted degradation strategies for therapeutic applications. -
IKZF1/3 And CSNK1A1 Molecular Glue Degrader
MI-2-80 is a molecular glue degrader that specifically targets IKZF1 and IKZF3, as well as CSNK1A1. This compound facilitates the binding of these proteins to the cereblon (CRBN) E3 ubiquitin ligase, promoting their subsequent ubiquitination and proteasomal degradation. MI-2-80 is valuable for research applications focused on understanding the functional roles of IKZF proteins and their involvement in various pathologies, including hematological malignancies. -
p300/CBP Inhibitor
KB528 is a selective inhibitor of the histone acetyltransferases p300 and CBP, demonstrating low nM IC50 values against these targets while sparing other members of the KAT family. This compound modulates the IRF4 transcriptional network, leading to decreased expression of key oncogenes such as IRF4, MYC, CAV2, and IGLL5, as well as reduced levels of IKZF3 protein. KB528 has been shown to effectively induce apoptosis in multiple myeloma cells, making it a valuable tool for research in multiple myeloma and related oncological studies. -
IKZF Degrader
BMS-986482 is a CRBN-mediated IKZF degrader that selectively targets the IKZF1-4 protein family. Its unique CELMoD™ core facilitates the degradation of these proteins, leading to impaired tumor growth as demonstrated in preclinical mouse models. This compound is particularly valuable for research focused on advanced solid tumors, providing insights into therapeutic strategies that disrupt IKZF protein function. -
HIV-1 Nef Binder, IKZF1 Modulator
FC-14369 is a PROTAC degrader that selectively targets the HIV-1 Nef protein, exhibiting a DC50 value of 160 nM. By engaging both Nef and the Cereblon E3 ubiquitin ligase, FC-14369 facilitates the ubiquitination and subsequent proteasomal degradation of Nef, leading to the restoration of CD4 and MHC-I expression on the cell surface and effectively inhibiting HIV-1 replication. This compound is valuable for research focused on HIV infection and AIDS, advancing understanding of therapeutic strategies in viral infections. -
CRBN Degrader
WDR5 Degrader-1 is a cereblon (CRBN)-recruiting compound designed to selectively induce degradation of the WDR5 protein. This degrader effectively targets WDR5 while sparing the CRBN neo-substrate IKZF1, facilitating precise manipulation of WDR5 levels in cellular systems. It is a valuable tool for investigating the biological roles of WDR5 in transcriptional regulation and potential therapeutic strategies in diseases associated with dysregulated WDR5 expression. -
IKZF2 degrader
NVP-DKY709 is an orally active molecular glue degrader targeting IKZF2. This compound demonstrates a Dmax of 53% and a DC50 of 4 nM, indicating potent degradation efficacy. Additionally, NVP-DKY709 can also degrade IKZF4 and SALL4 with DC50 values of 13 nM and 2 nM, respectively. Its mechanism involves binding to CRBN, altering its conformation to facilitate the recruitment and degradation of IKZF2, thereby exerting significant anti-tumor activity. This functionality positions NVP-DKY709 as a valuable tool in cancer research and therapeutic development targeting IKZF protein family members. -
PROTAC IKZF1/3 Degrader
Cemsidomide is a PROTAC degrader targeting IKZF1 and IKZF3, utilizing the ubiquitin ligase pathway. It exhibits potent biological activity with a GI50 of 0.05 nM against NCIH929.1 cells. This compound is primarily employed in the exploration of multiple myeloma (MM) research, facilitating the study of targeted protein degradation in cancer therapeutics. -
IKZF2 Molecular Glue Degrader
PLX-4545 is an orally active and selective molecular glue degrader that targets IKZF2 (zinc finger transcription factor Helios) via cereblon. This compound reprograms immunosuppressive regulatory T cells into pro-inflammatory effector T cells, thereby enhancing anti-tumor immune responses. PLX-4545 is intended for research applications related to solid tumors and the modulation of T cell functionality. -
IKZF2 Molecular Glue Degrader
(S,S)-PLX-4545 is a cereblon-based molecular glue degrader targeting IKZF2, a zinc finger transcription factor involved in immune regulation. This compound effectively promotes the degradation of IKZF2, making it a valuable tool for investigating IKZF2-related diseases, including various proliferative disorders and cancers. Researchers can leverage (S,S)-PLX-4545 to explore therapeutic strategies targeting IKZF2 functionality in different biological contexts. -
Enantiomer Of PLX-4545
(1S,2S,3R)-PLX-4545 is the (1S,2S,3R) enantiomer of PLX-4545, functioning as a selective cereblon-based molecular glue degrader that targets IKZF2 (zinc finger transcription factor Helios). This compound effectively reprograms immunosuppressive regulatory T cells into pro-inflammatory effector T cells, enhancing anti-tumor immune responses. Its applications extend to immunology and cancer research, providing insights into T cell modulation and potential therapeutic strategies for cancer immunotherapy. -
IKZF2 Selective and orally Inhibitor
PVTX-405 is a selective, orally bioavailable inhibitor targeting IKZF2, designed as a molecular glue degrader. With a DC50 of 0.7 nM and a Dmax of 91%, it enhances degradation efficiency while minimizing off-target effects, exhibiting an IC50 of 48 µM for hERG inhibition. PVTX-405 demonstrates significant antitumor activity by inhibiting the growth of MC38 tumors and shows improved efficacy when combined with immune checkpoint therapies, such as anti-PD1 or anti-LAG3, in mouse models. -
IKAROS Protein Degrader
MGD-4 is an orally bioavailable IKAROS protein degrader that operates via Cereblon (CRBN) dependence, demonstrating effective degradation of IKZF1 (DC50=67.2 nM), IKZF2 (DC50=918.2 nM), and IKZF3 (DC50=95.8 nM). It exhibits significant anti-proliferative activity against multiple myeloma, making it a valuable tool for research into therapies targeting hematological malignancies. This compound is ideal for studies investigating the role of IKAROS family proteins in cancer biology and the development of protein degradation strategies. -
USP3 ZnF-UBD Ligand
USP3 ZnF-UBD Ligand-1 is a small molecule that specifically targets the zinc finger ubiquitin-binding domain (ZnF-UBD) of USP3, exhibiting a binding affinity characterized by a KD of 14 μM. This ligand can be utilized in studies investigating the role of USP3 in ubiquitin signaling pathways and its implications in various diseases. Its ability to selectively bind to USP3 enables researchers to explore potential therapeutic strategies targeting this deubiquitinating enzyme. -
Molecular Glue IKZF2-Degrader
IKZF2-degrader 3 is a molecular glue that selectively targets and degrades the IKZF2 protein, exhibiting a DC50 of 2.0 nM. It enhances the understanding of IKZF2's role in various biological processes and is useful for studying its implications in hematological malignancies. This reagent is valuable for research focused on targeted protein degradation and its therapeutic potential in cancer treatment. -
IKZF1 Degrader
IKZF1-degrader-2 is a molecular glue degrader that specifically targets IKZF1, facilitating its degradation in cancer cells. This compound exhibits potent anticancer activity while demonstrating low toxicity, making it a valuable tool for oncology research. IKZF1-degrader-2 is ideal for studies focused on targeted protein degradation and its therapeutic implications in cancer treatment. -
IKZF2 Degrader
IKZF2-degrader 2 is a selective molecular glue degrader that targets IKZF2, facilitating its ubiquitination and subsequent degradation through recruitment of the CRL4-CRBN E3 ubiquitin ligase. With DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS assays, respectively, this compound also induces moderate degradation of SALL4 (DC50 of 9 nM) without significantly affecting IKZF1, IKZF3, CK1α, or GSPT1. IKZF2-degrader 2 is suitable for investigating mechanisms in cancer immunology. -
IKZF2 Molecular Glue Degrader
IKZF2-degrader 1 is a selective IKZF2 molecular glue degrader that exhibits a DC50 of 0.5 nM, effectively targeting IKZF2 for degradation. With minimal activity against CK1α (DC50: 210 nM), it provides a focused approach for studying the role of IKZF2 in cellular processes. This compound is valuable for researching IKZF2-dependent cancers, enabling investigations into its therapeutic potential and biological mechanisms. -
PROTAC Target Protein Ligand
IKZF1/3 ligand-1 is a PROTAC target protein ligand designed for the synthesis of PROTACs, specifically the PROTAC IKZF1/3 Degrader-1. This compound exhibits potent degradation activity against IKZF1 and IKZF3, making it a valuable tool in neuroprotective research applications. Its mechanism supports the targeted degradation of IKZF proteins, facilitating studies into their roles in various biological processes and disease pathways. -
IKZF2 Degrader
IKZF2-degrader 4 is an IKZF2-targeting compound that facilitates the degradation of the IKZF2 protein. Through its mechanism, this degrader can disrupt the function of IKZF2, which is implicated in various cancer pathways. It is a valuable tool for investigating IKZF2's role in tumor biology and for exploring therapeutic strategies in cancer research. -
IKZF1 Degrader
IKZF1-degrader-1 is a molecular glue degrader targeting IKZF1, with a DC50 value of 0.134 nM. This compound facilitates the selective degradation of IKZF1, making it a valuable tool for research into tumor biology and potential cancer therapies. Its ability to modulate IKZF1 levels may provide insights into the role of this transcription factor in oncogenesis and therapeutic resistance. -
PROTAC IKZF1/IKZF3 Degrader
(Rac)-Cemsidomide is a PROTAC degrader targeting IKZF1 and IKZF3, exhibiting potent antitumor activity through its molecular glue mechanism. This compound demonstrates a GI50 of 0.05 nM in NCIH929.1 cells, making it a valuable tool for research applications focused on the degradation of Ikaros and Aiolos proteins. Its unique properties facilitate investigations into mechanisms of action related to targeted protein degradation in cancer therapies. -
PROTAC Linker
tert-Butyl 6-aminocaproate is a PROTAC linker that facilitates the development of targeted protein degraders. This compound plays a crucial role in the synthesis of PROTAC CARM1/IKZF3 degrader-1, enabling selective degradation of target proteins. Its utility in chemical research supports the exploration of innovative therapeutic strategies through targeted protein modulation. -
Immunomodulatory/Antineoplastic Agent
Lenalidomide hydrochloride is an oral immunomodulatory agent targeting cereblon (CRBN), acting as a molecular glue. It promotes the selective ubiquitination and degradation of transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 ubiquitin ligase complex. This mechanism effectively inhibits the growth of mature B-cell lymphomas, including multiple myeloma, while also inducing the release of IL-2 from T cells, making it valuable in cancer research and therapeutic applications. -
E3 Ligase Ligand-Linker Conjugate
Thalidomide-NH-C4-Boc is a conjugate that targets the E3 ligase Cereblon through an innovative linker. This compound facilitates the synthesis of PROTAC CARM1/IKZF3 degrader-1, enabling targeted protein degradation studies. Its primary application lies in the development of novel therapeutics and novel molecular probes in cellular research. -
Thrombin Inhibitor
PPACK dihydrochloride is a potent and selective irreversible inhibitor of thrombin. It serves as an alternative anticoagulant to lithium heparin for blood gas and electrolyte analyses in whole blood. Additionally, PPACK dihydrochloride inhibits plasminogen activator (rt-PA), preventing its binding to plasma protease inhibitors. This compound also reduces plasmin-induced endothelial permeability and morphological changes in bovine aortic endothelial cell monolayers, making it suitable for investigations in thrombosis-related research. -
CRBN Inhibitor
EM12-SO2F is a potent covalent inhibitor of the E3 ubiquitin ligase cereblon (CRBN), specifically binding to the histidine residue at position 353. This compound serves as a valuable chemical probe for studying CRBN-mediated pathways. EM12-SO2F effectively inhibits the lenalidomide-induced degradation of IKZF1 in MOLT4 cells, making it a useful tool for research in cancer biology and drug resistance.
