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PROTAC degraders recruit an E3 ubiquitin ligase to a target protein so that the proteasome degrades it. Each proteolysis-targeting chimera (PROTAC) links a target-binding ligand to an E3 ligase ligand through a chemical linker. The approach was first described in 2001, and later work showed that small-molecule PROTACs can act catalytically, removing several target copies per molecule. Examples include the bromodomain and extra-terminal (BET) degraders dBET1, MZ1 and ARV-771, and the estrogen receptor degrader ERD-308. Degraders of anti-apoptotic proteins, such as PROTAC Mcl1 degrader-1, are also listed.
PROTAC BTK Degrader-3 is a selective degrader targeting Bruton's tyrosine kinase (BTK) with a DC50 value of 10.9 nM for BTK degradation in Mino cells. This compound demonstrates significant biological activity and is applicable in research focusing on B-cell malignancies, particularly chronic lymphoid malignancies. Its mechanism of action offers potential pathways for therapeutic intervention in relevant disease models.
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PROTAC BTK Degrader-9 functions as a targeted degrader of Bruton's tyrosine kinase (BTK), primarily inhibiting the NFAT signaling pathway. By downregulating the BTK-PLCγ2-Ca2+-NFATc1 cascade activated by RANKL, it demonstrates significant potential in inhibiting osteoclastogenesis and reducing alveolar bone loss. This compound is suitable for research applications related to bone resorption and inflammation in models of periodontitis.
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PROTAC BTK Degrader-14 is a targeted protein degrader that specifically degrades Bruton's tyrosine kinase (BTK) through the PROTAC mechanism of action. This compound is significant in cancer research, particularly for studies focused on malignancies where BTK plays a crucial role in signaling pathways. Its ability to effectively modulate BTK levels can provide insights into therapeutic strategies and disease mechanisms involving this key protein.
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SIAIS001 is a potent PROTAC degrader targeting anaplastic lymphoma kinase (ALK) with a DC50 of 3.9 nM. This compound induces G1/S phase cell cycle arrest and effectively inhibits the proliferation of SR cells with an IC50 of 0.9 nM. SIAIS001 is suitable for research in non-small cell lung cancer (NSCLC) and anaplastic large-cell lymphomas (ALCLs).
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Synonyms: Gal-MS99
MS99-β-Gal is a galactose-modified PROTAC degrader targeting the NPM-ALK fusion protein. This compound is selectively hydrolyzed by SA-β-gal and esterase in senescent cancer cells, allowing the release of MS99, which effectively degrades the NPM-ALK protein. MS99-β-Gal demonstrates an IC50 of 454.8 nM in aging Karpas 299 cells, showing improved potency compared to normal Karpas 299 cells with an IC50 of 2.162 μM. This reagent is valuable for cancer research, particularly in studies focused on targeted protein degradation.
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PROTAC EML4-ALK Degrader-2 is an advanced degrader specifically targeting the EML4-ALK fusion protein. With an IC50 of 1.6 nM, it exhibits potent selective inhibitory activity against ALK while maintaining selectivity over IGF1R, INSR, FLT3, and FGFR2. This compound demonstrates significant anti-cancer effects in both in vitro and in vivo models and is particularly relevant for research applications involving non-small cell lung cancer (NSCLC), as well as liver and cervical cancers.
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SIAIS117 is a potent Brigatinib-PROTAC degrader that targets the ALK protein, specifically effective against the ALK G1202R point mutation. By utilizing a VHL-1 conjugation, SIAIS117 exhibits significant capability to induce protein degradation, leading to inhibited growth of SR and H2228 cancer cell lines. This compound holds potential for applications in anti-proliferative research, particularly in small cell lung cancer contexts.
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PROTAC ALK degrader-5 is a targeted degrader composed of a small molecule that selectively degrades anaplastic lymphoma kinase (ALK). It demonstrates potent inhibitory activity against EML4-ALK and NPM-ALK, with IC50 values of 27.4 nM and 116.5 nM, respectively. This compound exhibits significant anti-proliferative effects against ALK-driven cancer cell lines, including H3122 and Karpas 299, and effectively inhibits ALK and STAT3 phosphorylation. PROTAC ALK degrader-5 is a valuable tool for investigating ALK-driven malignancies, particularly in the context of human non-small cell lung cancer and anaplastic large cell lymphoma research.
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TD-004 is a highly effective ALK PROTAC degrader, demonstrating potent anti-ALK inhibitory activity with an IC50 of 0.11 µM. This compound selectively hampers the proliferation of ALK-positive cancer cell lines, SU-DHL-1 and H3122, with IC50 values of 0.058 µM and 0.28 µM, respectively. TD-004 induces the degradation of ALK fusion proteins, including NPM-ALK and EML4-ALK, through the recruitment of the VHL E3 ligase and the proteasome pathway. Its significant tumor growth inhibition and favorable safety profile in vivo make TD-004 a valuable tool for researching anaplastic large cell lymphoma and non-small cell lung cancer.
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PROTAC VEGFR-2 Degrader-1 is a targeted protein degradation compound designed to selectively degrade VEGFR-2. It demonstrates minimal VEGFR-2 inhibition with an IC50 exceeding 1 μM, and exhibits limited anti-proliferative activity against EA.hy926 cells, with an IC50 greater than 100 μM. This reagent is valuable for research applications focused on the regulation of VEGFR-2 and its role in vascular biology and related disease mechanisms.
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PROTAC VEGFR-2 Degrader-2 primarily targets the vascular endothelial growth factor receptor 2 (VEGFR-2) for degradation through the PROTAC mechanism. This compound displays minimal inhibition of VEGFR-2 activity with an IC50 exceeding 1 μM and demonstrates anti-proliferative effects in EA.hy926 cells, with an IC50 greater than 100 μM. It serves as a valuable tool for studies focused on targeted protein degradation and the modulation of signaling pathways related to angiogenesis.
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BLK Degrader 1 is a selective degrader of B-lymphoid tyrosine kinase (BLK), a key regulator in B-cell signaling pathways. This compound exhibits significant anticancer activity across various B-lymphoid cell lines, making it a valuable tool for research into B-cell malignancies. Its targeted degradation of BLK offers potential insights into therapeutic strategies for treating cancers that involve B-lymphoid cells.
SJ45566 is a potent PROTAC-based degrader targeting LCK with a DC50 of 1.21 nM. This compound is designed for the selective degradation of LCK, providing a valuable tool for investigating T-Cell Acute Lymphoblastic Leukemia. Its efficacy in modulating LCK levels makes it applicable in studies aimed at understanding T-cell signaling pathways and cancer biology.
LCK Degrader-3 is a CRBN-based molecular glue degrader targeting LCK (lymphocyte-specific protein tyrosine kinase). This compound facilitates the selective degradation of LCK, making it a valuable tool for investigating the role of LCK in acute lymphoblastic leukemia. Its application in research may provide insights into therapeutic mechanisms and potential treatment strategies for leukemia.
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NTRK Degrader-1 is a potent PROTAC degrader specifically targeting both wild-type and mutant NTRK1, with IC50 values of 4 nM for wild-type, 2 nM for G595R, 5 nM for G667C, and
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CG428 is a potent CRBN-dependent PROTAC degrader specifically targeting tropomyosin receptor kinase (TRK). It effectively reduces levels of the TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells with a DC50 of 0.36 nM and inhibits downstream PLCγ1 phosphorylation with an IC50 of 0.33 nM. CG428 demonstrates higher binding affinity for TRKA (Kd = 1 nM) compared to TRKB and TRKC, making it a valuable tool for research into colorectal carcinoma.
PROTAC RET Degrader 1 is an orally bioavailable RET PROTAC degrader that effectively crosses the blood-brain barrier. It demonstrates remarkable potency with DC50 values for various RET mutations, including 1.7 nM for RET (WT) and 3 nM for RET (G810S). PROTAC RET Degrader 1 exhibits strong anti-proliferative effects in cancer cell lines harboring oncogenic RET fusions and mutations, and shows significant anti-tumor efficacy in patient-derived xenograft mouse models. This reagent is valuable for investigating RET-positive cancers and their therapeutic targeting.
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PROTAC IRAK4 degrader-13 is a selective IRAK4-directed PROTAC degrader that effectively targets IRAK4 with DC50 values of 0.86 nM and 1.1 nM in monocytes and lymphocytes, respectively. This compound significantly activates TIR signaling and reduces the expression of proinflammatory cytokines in an Imiquimod-induced psoriasis mouse model. PROTAC IRAK4 degrader-13 is applicable in research focused on TLR- and IL-1R-driven inflammatory diseases, including hidradenitis suppurativa and atopic dermatitis.
PROTAC PD-L1 degrader-2 is a selective degrader targeting PD-L1. It demonstrates a potent inhibitory effect with an IC50 of 197.4 nM and a binding affinity characterized by a Kd of 301 nM. This compound facilitates the internalization and subsequent degradation of PD-L1 through both proteasomal and lysosomal pathways, thereby enhancing immune system activation. Its efficacy has been validated in MC38 C57BL/6 mouse models, underscoring its potential for antitumor applications.
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PROTAC HPK1 Degrader-5 is a highly potent and orally bioavailable PROTAC that targets HPK1 for degradation (DC50 = 5.0 nM; Dmax ≥ 99%). This compound effectively inhibits SLP76 phosphorylation and promotes ERK pathway activation, leading to increased release of IL-2 and IFN-γ. It demonstrates the capability to counteract immunosuppressive signals induced by PGE2, NECA, or TGF-β. Additionally, PROTAC HPK1 Degrader-5 has shown efficacy in inhibiting tumor growth in MC38 syngeneic mouse models, making it a valuable tool for research in tumor immunotherapy, particularly in colorectal cancer.
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PROTAC IRAK4 degrader-14 is an orally active degrader targeting IRAK4 with a DC50 of 2.4 nM. It functions by selectively degrading IRAK4, thereby inhibiting pro-inflammatory responses in various cell types, including T cells, monocytes, and keratinocytes. This compound has significant relevance in research focused on inflammatory diseases, particularly psoriasis.
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PVD-06 is a selective PROTAC degrader targeting PTPN2, exhibiting a DC50 of 217 nM with a selectivity index greater than 60-fold over PTP1B. This compound facilitates the degradation of PTPN2 through a VHL-, ubiquitin-, and proteasome-dependent mechanism. It has been shown to enhance T cell activation and promote IFN-γ-mediated anticancer effects. PVD-06 is a valuable tool for exploring the role of PTPN2 in various diseases, including leukemia and melanoma.
JCS-1 is a highly potent DcpS PROTAC degrader that facilitates the targeted degradation of the DcpS enzyme through non-covalent binding via a RG3039-based warhead, while recruiting the E3 ligase VHL. This compound effectively promotes ubiquitination and subsequent degradation of DcpS at nanomolar concentrations, demonstrating a DC50 value of 87 nM in MOLM-14 cells. JCS-1 is a valuable tool for investigating acute myeloid leukemia (AML) and other genetic disorders associated with DcpS dependency.
PROTAC PTPN2 degrader-2 TFA is a highly potent PTPN2 degrader with a DC50 of less than 50 nM. This compound facilitates targeted protein degradation, providing a valuable tool for investigating the role of PTPN2 in cancer and metabolic disorders, including colon cancer. Its application in research can enhance understanding of disease mechanisms and therapeutic interventions.
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PROTAC PTPN2 Degrader-2 is a selective PTPN2 degrader that effectively induces targeted degradation of the PTPN2 protein, demonstrating a DC50 of less than 50 nM. This compound is instrumental for exploring cellular mechanisms within cancer and metabolic disorders, particularly in the context of colon cancer research. Its utility in protein knockdown enables innovative studies into therapeutic strategies for disease intervention.
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