PROTACs
PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.
PROTACs Isoform Specific Products
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PROTACs Related Products (1398)
Related Products (1398)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC SOS1 degrader-5
0 ImagesCat. No.: HY-161173CAS No.: 2836273-61-9PROTAC SOS1 degrader-5 is a potent SOS1 PROTAC degrader with a DC50 value of 13 nM. PROTAC SOS1 degrader-5 induces CRBN-dependent ubiquitination and degradation of SOS1 protein, inhibits the proliferation of KRASG12C-mutated cancer cells, and suppresses tumor growth in xenograft models. PROTAC SOS1 degrader-5 can be used in studies related to KRASG12C-mutated non-small cell lung cancer.
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PROTAC BRD2/BRD4 degrader-1
0 ImagesCat. No.: HY-130612CAS No.: 2570470-42-5PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect.
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SK5527
0 ImagesCat. No.: HY-179641CAS No.: 3131860-12-0SK5527 is a selective AURKA PROTAC degrader degrading AURKA with DC50 = 2 nM. SK5527 bind to NanoLuc-AURKA with an IC50 of 20 nM. SK5527 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK5527 efficiently reduced AURKA levels in vivo. SK5527 can be used for neuroblasto2ma research.
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PROTAC FAK degrader 3
0 ImagesCat. No.: HY-175459PROTAC FAK degrader 3 is a potent and selective FAK PROTAC degrader with a DC50 of 1.08 nM. PROTAC FAK degrader 3 induces the ubiquitination and proteasomal degradation of FAK by binding to CRBN, thereby blocking oncogenic signaling, specifically upregulating MHC-I to enhance antigen presentation, and subsequently activating CD8+ T cell-mediated antitumor immune responses. PROTAC FAK degrader 3 can be used in related research on hepatocellular carcinoma, ovarian cancer, and breast cancer.
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PROTAC SMARCA2 degrader-36
0 ImagesCat. No.: HY-181909PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers.
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PROTAC BRD4 Degrader-33
0 ImagesCat. No.: HY-174811PROTAC BRD4 Degrader-33 is a BRD4 PROTAC degrader that recruits CRBN. PROTAC BRD4 Degrader-33 downregulates PD-L1 expression, inhibits tumor cell proliferation and tumor growth in mice by inducing ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-33 can be used in the research of breast cancer.
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PROTAC FLT-3 degrader 4
0 ImagesCat. No.: HY-158325CAS No.: 2956722-48-6PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor).
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PROTAC METTL3-14 degrader 1
0 ImagesCat. No.: HY-162282CAS No.: 3039554-79-2PROTAC METTL3-14 degrader 1 is a METTL3-METTL14 heterodimer complex PROTAC degrader. PROTAC METTL3-14 degrader 1 binds to the E3 ubiquitin ligase CRBN, forms a ternary complex with METTL3-METTL14, and promotes the ubiquitination and degradation of METTL3. PROTAC METTL3-14 degrader 1 is applicable to the research of acute myeloid leukemia and prostate cancer.
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PROTAC BRD4 Degrader-21
0 ImagesCat. No.: HY-156566CAS No.: 2503036-46-0PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma.
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SH-26
0 ImagesCat. No.: HY-183995SH-26 is a PHD1 PROTAC degrader with DC50s of 1.06 μM, 4.16 μM and 4.91 μM in MDA-MB-231, HepG2 and HEK-293T cells, respectively. SH-26 recruits CRBN to induce PHD1 degradation via the ubiquitin-proteasome system. SH-26 attenuates APAP (HY-66005)-triggered ROS accumulation, mitochondrial dysfunction, and NLRP3 inflammasome activation. SH-26 can be used for the research of acute liver injury.
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OICR41114
0 ImagesCat. No.: HY-169389OICR41114 is a WDR5 PROTAC degrader with an EC50 of 40 nM. OICR41114 binds both DCAF1 and WDR5, and its binding affinity for DCAF1 is significantly enhanced in the presence of WDR5 (KD increases from 59 nM to 5 nM). OICR41114 exerts antiproliferative effects on MV4-11 cells. OICR41114 can be used for the research of acute myeloid leukemia.
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PROTAC MAGL degrader-1
0 ImagesCat. No.: HY-173369PROTAC MAGL degrader-1 is an orally active, moderately blood-brain barrier permeable bifunctional PROTAC (DC50: 60.28 nM) that possesses MAGL degradation activity alongside MDM2 inhibitory activity. PROTAC MAGL degrader-1 recruits E3 ubiquitin ligase MDM2 to mediate ubiquitination of MAGL and subsequent proteasomal degradation. PROTAC MAGL degrader-1 blocks the interaction between MDM2 and P53 and upregulates the expression of tumor suppressor protein P53. PROTAC MAGL degrader-1 is applicable for research on glioblastoma stem cells, melanoma and breast cancer.
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Lw13
0 ImagesCat. No.: HY-162589Lw13 is a Hsp90 PROTAC degrader. Lw13 induces Hsp90 degradation via the ubiquitin-proteasome system, destabilizes client proteins HER2 and AKT, and blocks the activation of the HER2/AKT/mTOR signaling pathway. Lw13 inhibits the metastasis of cervical cancer cells, induces cell cycle arrest and apoptosis (apoptosis). Lw13 exerts synergistic anti-tumor activity with Cisplatin (HY-17394). Lw13 is applicable to cervical cancer-related research.
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PROTAC PLK1 Degrader-3
0 ImagesCat. No.: HY-181000CAS No.: 3074520-74-1PROTAC PLK1 Degrader-3 (Compound DD-1) is a PLK1 PROTAC degrader based on the N-deglycosylation pathway, with a Kd value of 2.2 μM. The cell penetration ability of PROTAC PLK1 Degrader-3 is limited and a higher concentration is required to achieve significant degradation effects. PROTAC PLK1 Degrader-3 can be used for research on non-small cell lung cancer.
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G6374
0 ImagesCat. No.: HY-180787G6374 is a IRE1 PRORAC degrader with DC50 values of 0.04 μM (AMO1) and 0.13 μM (KMS27), an EC50 value of 0.11 μM, and KD values of 0.56 nM and 90.2 nM for IRE1 and VHL, respectively. G6374 binds to the ATP pocket of the IRE1 kinase domain and VHL to form a ternary complex that recruits CRL2VHL, inducing K48-linked polyubiquitination of IRE1 at lysine residues K704 and K717, which in turn drives proteasomal degradation of monomeric and dimeric IRE1. G6374 can be used for the research of multiple myeloma.
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CP-07
0 ImagesCat. No.: HY-149495CP-07 is a selective flavonoid-based PROTAC degrader that targets and degrades CDK9. CP-07 exhibits an IC50 of 3.3 nM against CDK9/cyclin T1, and induces CDK9 degradation in a concentration-dependent manner in 22RV1 cells with a DC50 of 43 nM. CP-07 rapidly triggers ligand-dependent and proteasome-dependent degradation of CDK9. CP-07 can be applied in prostate cancer-related research.
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PROTAC HDAC6 degrader 6
0 ImagesCat. No.: HY-174877CAS No.: 3068162-16-0PROTAC HDAC6 degrader 6 is a HDAC6 PROTAC degrader that recruits CRBN, and also a photoactivatable photochemical targeting chimeric (PHOTAC). PROTAC HDAC6 degrader 6 switches between cis and trans conformations upon illumination, in which the cis conformation binds HDAC6 and CRBN to form a ternary complex, and induces HDAC6 degradation via ubiquitin-like modification, polyubiquitination and proteasomal pathways. PROTAC HDAC6 degrader 6 can be used in the research of multiple myeloma.
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PROTAC STING Degrader-2
0 ImagesCat. No.: HY-158036CAS No.: 3023095-61-3PROTAC STING Degrader-2 is a STING PROTAC degrader with a DC50 of 0.53 μM. PROTAC STING Degrader-2 reduces the phosphorylation levels of TBK1 and IRF3. PROTAC STING Degrader-2 decreases the mRNA expression levels of IFN-β, CXCL10 and TNF-α, and blocks luciferase secretion. PROTAC STING Degrader-2 can be used in the research of autoimmune diseases.
