- Cyclosporin A (Cyclosporine A) is an immunosuppressant agent widely used in post-allogeneic organ transplant to reduce the activity of the immune system.
- X Jia, .et al. , J Hazard Mater, 2020, Jun 4;399:123034 PMID: 32544768
- Y Huang, .et al. , Experimental and Therapeutic Medicine, 2020, 20(2), 736-747 PMID: 32742319
- Miyayama Y, .et al. , Microbiol Immunol, 2019, Dec 19 PMID: 31854467
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Ubiquitin ligase inducer
Lenalidomide is a derivative of thalidomide. In vitro, lenalidomide has three main activities: direct anti-tumor effect, inhibition of the micro environment support for tumor cells, and immunomodulatory role. It induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity.- Kazuya Ishiguro, .et al. , Cancer Lett, 2025, Oct 28:631:217941 PMID: 40701319
- Sumie Fujii, .et al. , Stem Cells and Development, 2025, 34: 9-10
- Daniel A. Rauch, .et al. , Retrovirology, 2020, 17: 27 PMID: 32859220
- A Hayano, .et al. , Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Kumar R, .et al. , Mol Biol Rep, 2018, Oct 11 PMID: 30311125
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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TNF-alpha inhibitor
Pomalidomide is a derivative of thalidomide and acts as an immunomodulator. -
Cereblon E3 Ubiquitin Ligase Modulating Agent
CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD). CC-92480 shows high affinity to cereblon, resulting in potent antimyeloma activity. -
BTK/GSPT1 Degrader
GBD-9 is a dual-action degrader that targets both BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). It acts as a PROTAC to promote BTK degradation and functions as a molecular glue to induce GSPT1 degradation. GBD-9 exhibits significant antiproliferative activity in cancer cells, making it a promising candidate for cancer research. - Tz-Thalidomide is a tetrazine-tagged thalidomide derivative that functions as a ligand for E3 ligases. It exhibits binding affinity for BRD4, with IC₅₀ values of 46.25 μM for BRD4-1 and 62.55 μM for BRD4-2. As a click chemistry reagent, Tz-Thalidomide contains a tetrazine moiety capable of undergoing inverse electron demand Diels–Alder (iEDDA) reactions with trans-cyclooctene (TCO)-containing molecules, enabling bioorthogonal labeling and conjugation applications.
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GSPT1 degrader
LYG-409 is an orally active degrader of GSPT1 that demonstrates potent antitumor activity in vivo, with tumor growth inhibition (TGI) rates of 94.34% in acute myeloid leukemia and 104.49% in prostate cancer models. In vitro, LYG-409 inhibits KG-1 cells through GSPT1 degradation, with an IC₅₀ of 9.50 nM and a DC₅₀ of 7.87 nM. -
Molecular glues
ERAS-0015 (Pan-RAS-IN-2) is a molecular glue that targets RAS by promoting the formation of ternary complexes with cyclophilin A (CYPA) and active RAS (ON) proteins. This interaction disrupts the binding of RAF to RAS, thereby inhibiting downstream signaling. Pan-rasin-2 exhibits significant antiproliferative activity in RAS-mutant cell lines and shows promise as an anti-tumor agent. -
two-site molecular glue
LL-K12-18 is a two-site molecular glue that enhances the protein-protein interaction between CDK12 and DDB1, stabilizing the complex and promoting cyclin K degradation with an EC50 of 0.37 nM. It exhibits potent transcriptional repression and anti-proliferative activity in tumor cells, making it a valuable tool for cancer research. -
CK1α degrader
TMX-4116 is a selective degrader of casein kinase 1α (CK1α), demonstrating preferential degradation activity with DC₅₀ values below 200 nM in MOLT4, Jurkat, and MM.1S cell lines. By targeting CK1α for proteasomal degradation, TMX-4116 offers a promising tool for investigating CK1α function and holds potential for therapeutic research in multiple myeloma and related hematologic malignancies. -
CK1α molecular glue degrader
SJ3149 is a selective and potent molecular glue degrader that targets casein kinase 1α (CK1α) for proteasomal degradation. By promoting CK1α elimination, SJ3149 exhibits broad antiproliferative activity across various cancer models. It serves as a valuable tool for exploring CK1α-dependent signaling pathways and holds promise for therapeutic development in oncology research. -
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. -
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). -
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. -
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. -
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 Glue Degrader
BTX306 is a cereblon-targeting molecular glue degrader that effectively reduces myeloma cell viability and induces apoptosis. This compound demonstrates the ability to overcome resistance in myeloma cells to traditional therapies such as Lenalidomide and Bortezomib. Additionally, BTX306 displays potent activity against primary myeloma cells and exhibits substantial efficacy in in vivo models. This reagent is suitable for research focusing on myeloma and related therapeutic strategies. -
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. -
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. -
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. -
Molecular Glue GSPT1 Degrader
TD-522 is a potent and selective molecular glue targeting GSPT1 for degradation, exhibiting a DC50 of 0.269 nM. This compound demonstrates significant anti-proliferative activity and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cell lines. Additionally, TD-522 effectively suppresses tumor growth in a TMD-8 xenograft model. It is applicable for research focused on AML and DLBCL. -
CK1α Molecular Glue
BMS-986397 is a selective and orally active cereblon-based molecular glue degrader targeting casein kinase 1α (CK1α). This compound effectively induces apoptosis and cell cycle arrest in acute myeloid leukemia (AML) cells, positioning it as a valuable tool for research in the fields of AML and high-risk myelodysplastic syndromes (HR-MDS). Its unique mechanism offers potential for elucidating CK1α's role in these malignancies. -
CRY1 Molecular Glue Degrader
M47 is a molecular glue degrader that specifically targets Cryptochrome 1 (CRY1), promoting its degradation within the nucleus. This compound has been shown to enhance apoptosis in Ras-transformed P53-deficient mouse skin fibroblast lines and prolong lifespan in p53 knockout mice. M47 serves as a valuable tool for research focused on cancer biology and the mechanisms of targeted protein degradation. -
Molecular Glue
(R)-CR8 trihydrochloride is a potent inhibitor of CDK1, CDK2, CDK5, CDK7, and CDK9, functioning as a molecular glue degrader that targets cyclin K. With inhibitory activity characterized by low nanomolar IC50 values, it effectively induces apoptosis while exhibiting neuroprotective properties. This compound is suitable for research applications in cancer biology and neurodegenerative disease studies. -
Molecular Glues
(S)-Thalidomide is the S-enantiomer of Thalidomide, functioning as a molecular glue. It exerts significant biological activities, including immunomodulation, anti-inflammation, antiangiogenesis, and pro-apoptosis. This compound induces teratogenic effects through its interaction with cereblon (CRBN), making it a valuable tool for research into cell signaling pathways and developmental biology. -
CDK12/CCNK Molecular Glue
NCT02 is a molecular glue degrader that targets CDK12 through the E3 ubiquitin ligase DDB1, resulting in the ubiquitination and subsequent proteasomal degradation of its partner protein CCNK. This mechanism leads to the downregulation of CDK12, inhibiting its downstream signaling pathways. NCT02 exhibits significant biological activity by inducing apoptosis in tumor cells, arresting the cell cycle, and selectively inhibiting the proliferation of colorectal cancer cells with TP53 mutations or belonging to the CMS4 molecular subtype. Additionally, NCT02 demonstrates potential in suppressing tumor growth in both in vitro and in vivo models. -
Molecular Glue Degrader
VNPP433-3β is an orally active molecular glue degrader that targets androgen receptor (AR) and its splice variants (AR-Vs), as well as MAP kinase-interacting serine/threonine protein kinases Mnk1/2. This compound induces apoptosis in cells and demonstrates significant inhibition of tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β is a valuable tool for investigating mechanisms in castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
CCNK Molecular Glue Degrader
ZLY025 is a potent CCNK molecular glue degrader with a DC50 of 42.7 nM. This compound demonstrates significant antiproliferative effects across a range of tumor cell lines, exhibiting IC50 values between 0.08 and 2.45 μM. ZLY025 is capable of inducing apoptosis and causing G1 phase cell cycle arrest, making it a valuable tool for cancer research, particularly in the study of lung cancer. -
Molecular Glue Degrader
VNPP433-3β hydrochloride functions as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants, as well as MAP kinase-interacting serine/threonine protein kinases Mnk1 and Mnk2. This compound promotes apoptosis in cancer cells and has demonstrated efficacy in inhibiting tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride is suitable for research applications focused on castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
Molecular Glue Degrader
VNPP433-3β dihydrochloride is a potent molecular glue degrader that targets the androgen receptor (AR), AR splice variants (AR-Vs), and MAP kinase-interacting serine/threonine protein kinases Mnk1/2. This compound induces apoptosis in cancer cells and has been shown to inhibit tumor growth in CWR22Rv1 xenograft mouse models. VNPP433-3β dihydrochloride is valuable for research in castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
Molecular Glue Degrader
Galeterone hydrochloride is a potent molecular glue degrader that targets the androgen receptor (AR) and its splice variants, as well as MAP kinase-interacting serine/threonine protein kinases Mnk1/2. This compound also acts as a CYP17 inhibitor with an IC50 of 47 nM, promoting cell apoptosis and inhibiting tumor growth in human prostate cancer xenograft models. Galeterone hydrochloride is relevant in the research of castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
Molecular Glue
eEF2K degrader-2 is a molecular glue that targets the eEF2K protein, effectively mediating its degradation. This compound demonstrates significant biological activity by inhibiting proliferation, migration, and invasion, as well as inducing apoptosis in triple negative breast cancer (TNBC) cells. eEF2K degrader-2 exhibits minimal organ toxicity and pathological damage, making it a valuable tool for research applications focused on cancer biology, particularly in breast cancer studies. -
Lck Molecular Glue Degrader
LCK degrader-2 is a Lck molecular glue degrader designed to selectively target and degrade the Lck protein. This compound demonstrates potent biological activity in disrupting Lck-mediated signaling pathways, making it a valuable tool for studying acute lymphoblastic leukemia (ALL) and other Lck-dependent malignancies. Its application in cancer research provides insights into therapeutic strategies for Lck-related diseases. -
Molecular Glue
Lck degrader-1 is a molecular glue degrader that targets lymphocyte-specific protein tyrosine kinase (LCK) with a DC50 of 23.1 nM. This compound plays a significant role in the degradation of LCK, making it a valuable tool for studying T-cell acute lymphoblastic leukemia (T-ALL). Researchers can utilize Lck degrader-1 to explore the molecular mechanisms underlying T-ALL and investigate potential therapeutic strategies. -
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. -
CK1α molecular glue
dCK1α-2 is an orally active CK1α molecular glue degrader that targets proteins involved in the p53 signaling pathway. This compound demonstrates significant anti-tumor efficacy in preclinical mouse models and promotes the expression of p53-related genes, making it a valuable tool for research on cancer biology and therapeutic interventions aimed at restoring p53 function. Its mechanism of action provides insights into targeted degradation strategies in cancer treatment. -
CK1α Molecular Glue Degrader
QXG-6442 is a CK1α molecular glue degrader that effectively targets and degrades CK1α with a DC50 of 5.7 nM and a Dmax of 90%. This compound demonstrates significant antiproliferative effects in the MOLM-14 cell line, making it a valuable tool for research into the modulation of CK1α activity and its implications in various biological processes and diseases. -
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. -
STAT6 Molecular Glue
STAT6 degrader-1 is a bifunctional molecular glue that specifically targets STAT6 by recruiting E3 ubiquitin ligase, leading to the proteasomal degradation of the protein. This degradation mechanism allows for the modulation of STAT6 activity, making it a valuable tool in the study of cancer biology, inflammatory diseases, and colorectal cancer. Researchers can utilize STAT6 degrader-1 to explore therapeutic strategies aimed at disrupting STAT6 signaling pathways. -
Molecular Glue
OPB-171775 is an orally active molecular glue that targets phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). This compound induces SLFN12-mediated RNase activity, leading to subsequent cell death. Additionally, OPB-171775 activates the GCN2 signaling pathway associated with SLFN12, showcasing its significant efficacy in combating gastrointestinal stromal tumors. Researchers can utilize OPB-171775 to explore pathways in cancer biology and investigate the therapeutic potential of molecular glues in tumor treatment. -
Molecular Glue BRD4 Degrader
BRD4 degrader-1 is a monovalent, covalent molecular glue that specifically targets BRD4, a key regulator in various cellular processes. By engaging DCAF16, an E3 ubiquitin ligase, this compound facilitates the degradation of both long and short isoforms of BRD4 within the cellular context. Its mechanism of action makes BRD4 degrader-1 a valuable tool for research applications aimed at understanding and manipulating BRD4-related pathways in cancer and other diseases. -
Molecular Glue
AMPTX-1 is a molecular glue that functions as a selective, reversibly covalent degrader of BRD9, promoting its recruitment to the E3 ubiquitin ligase DCAF16. This compound exhibits significant activity in inducing proteasomal degradation of BRD9, making it a valuable tool for research involving chromatin regulation and cellular signaling pathways. AMPTX-1 can be utilized in studies focused on targeted protein degradation and the modulation of BRD9-related biological processes. -
SMARCA2/4 Molecular Glue Degrader
SMARCA2/4 degrader-1 is a molecular glue degrader specifically targeting SMARCA2 and SMARCA4, exhibiting a DC50 value of 2.2 nM for SMARCA4. This compound functions by covalently bridging CUL4DCAF16 and CRL1FBXO22, leading to the efficient degradation of SMARCA2 and SMARCA4 proteins. It is utilized in research to understand the roles of these proteins in various biological processes and disease states, particularly in cancer biology and epigenetic regulation. -
Molecular Glue BRD4 Degrader
BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue that selectively targets BRD4 for degradation by inducing a ternary complex with RNF126, an E3 ligase. This compound effectively promotes the degradation of both the long and short isoforms of BRD4 within cellular contexts. It serves as a valuable tool for investigating the roles of BRD4 in various biological processes and disease states, particularly in cancer research and therapeutic development. -
BRD9 Molecule Glue
BRD9 Degrader-3 is a molecular glue targeting BRD9, exhibiting a DC50 of less than 1.25 nM. This compound facilitates the proteolytic degradation of BRD9, effectively modulating protein levels within cellular systems. It is primarily utilized in research applications aimed at investigating the role of BRD9 in cancer biology and other disease contexts. -
RAF Molecular Glue
NST-628 is a molecular glue targeting RAF within the MAPK signaling pathway. It disrupts RAF phosphorylation and MEK activation by preventing the formation of BRAF-CRAF and BRAF-ARAF heterodimers. NST-628 exhibits significant biological activity in inhibiting RAS- and RAF-driven cancers, particularly in tumors with mutant KRAS, NRAS, BRAF class II/III, and NF1 mutations. This compound is a valuable tool for research into targeted cancer therapies and understanding the RAS-MAPK pathway's role in oncogenesis.

