HyT
Hydrophobie tagging
Hydrophobic tagging (HyT) 是一种通过在靶蛋白配体上引入疏水基团以模拟错误折叠蛋白、进而激活细胞蛋白质质量控制系统并诱导目标蛋白降解的新型靶向蛋白降解技术。由于其不依赖 E3 连接酶招募、分子量较小以及潜在的良好细胞通透性，HyT 已逐渐成为继 PROTACs 之后的重要蛋白降解策略。
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HyT Produits associés (18)
Produits associés (18)
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MS1943
0 ImagesMS1943 is an orally active selective HyT degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)).
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1-Adamantaneacetic acid
0 Images1-Adamantaneacetic acid is an aliphatic carboxylic acid that can be used as an acylating agent, commonly found in chemical synthesis.
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SARD279
0 ImagesCat. No.: HY-164807CAS No.: 1489236-55-6SARD279 is a potent and selective Androgen Receptor HyT degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research.
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ALK degrader 4
0 ImagesCat. No.: HY-182057CAS No.: 3111011-76-5ALK degrader 4 is a ALK HyT degrader with an IC50 of 0.74 nM. ALK degrader 4 inhibits ALK kinase activity, increases the solvent-accessible surface area of hydrophobic residues near the ALK binding pocket, promotes ALK to form a partially unfolded conformation, and induces proteasomal degradation of ALK. ALK degrader 4 inhibits cancer cell proliferation. ALK degrader 4 can be used in research related to non-small cell lung cancer (ALK ligand: Brigatinib (HY-12857); hydrophobic tag: Norbornene (HY-W013021)).
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JNK1 degrader-1
0 ImagesCat. No.: HY-182796JNK1 degrader-1 is a JNK1 HyT degrader. JNK1 degrader-1 can induce JNK1 degradation through the HyT-mediated ubiquitin-proteasome system and autophagy-lysosome pathway. JNK1 degrader-1 inhibits TGF-β1-induced epithelial-mesenchymal transition (EMT). JNK1 degrader-1 can be used for research on fibrotic diseases and cancer metastasis. (Pink: JNK1 ligand (HY-183006); Blue: Hyt hydrophobic group (HY-W037848); Black: Linker (HY-B1008)).
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Tetraasterane
0 ImagesCat. No.: HY-W1139353CAS No.: 259-77-8Tetraasterane is a hydrophobic tag that promotes the degradation of ALK protein. Tetraasterane can be used for synthesis of ALK degrader 3 (HY-182087).
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GPX4 degrader-1
0 ImagesCat. No.: HY-181598CAS No.: 3057531-85-5GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC50: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model.
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ALK degrader 2
0 ImagesCat. No.: HY-175527ALK degrader 2 is an orally active ALK HyT degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)).
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ALK degrader 1
0 ImagesCat. No.: HY-175849ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research.
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PARP1 degrader 1
0 ImagesCat. No.: HY-180276PARP1 degrader 1 (Compound 2c) is a comparatively potent PARP1 HyT degrader (DC50: 618 nM for intracellular PARP-1). PARP1 degrader 1 is also a HyT-Olaparib (HY-10162) conjugate. PARP1 degrader 1 induces UPR/autophagy, thus facilitating the degradation of PARP-1. PARP1 Degrader 1 can be used in the research of cancer.
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PARP1 degrader-2
0 ImagesCat. No.: HY-181460PARP1 degrader-2 (Compound 11e) is a potent, selective PARP1 HYT degrader (DC50: 2.16 μM). PARP1 degrader-2 selectively binds to and degrades PARP1 but not PARP2. PARP1 degrader-2 mediates the degradation of PARP1 via the ubiquitin-proteasome system (UPS). PARP1 degrader-2 exhibits anticancer activity against triple-negative breast cancer and colon cancer (hydrophobic tag: (HY-W022007); PARP1 ligand: (HY-75706); Linker: (HY-W015300)).
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ALK degrader 3
0 ImagesCat. No.: HY-182087ALK degrader 3 is a ALK HyT degrader with an IC50 of 1.2 nM. ALK degrader 3 inhibits ALK kinase activity, increases the solvent-accessible surface area of hydrophobic residues near the ALK binding pocket, promotes ALK to form a partially unfolded conformation, and drives ALK degradation via the proteasomal pathway. ALK degrader 3 inhibits the proliferation of tumor cells. ALK degrader 3 can be used for the research of non-small cell lung cancer. (ALK ligand: Brigatinib (HY-12857); hydrophobic tag: Tetraasterane (HY-W1139353)).
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5-Norbornene-2-methylamine-C10-NH2
0 ImagesCat. No.: HY-1819085-Norbornene-2-methylamine-C10-NH2 is a Keap1-targeting hydrophobic tag (HyT)-linker conjugates, containing a HyT (HY-W022007) and a linker (HY-W014831). 5-Norbornene-2-methylamine-C10-NH2 can be used for synthesis of NBE5 (HY-181907).
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NBE5
0 ImagesCat. No.: HY-181907NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C).
NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).
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ZX782
0 ImagesCat. No.: HY-161972ZX782 is a HyT GPX4 degrader and a ferroptosis inducer, which induces GPX4 degradation and significantly increases lipid ROS accumulation in HT1080 cells. ZX782 can be used to treat AD by reducing the size and/or number of brain amyloid plaques and by inhibiting the spread of IL-1beta-positive microglial-like cells around amyloid plaques. ZX782 is labeled with hydrophobic benzyl alcohol (HBA) and appears bright blue under acidic conditions, which can be used for quantitative determination. ZX782 is composed of target protein ligand (red part) ML-210 (HY-100003), PROTAC linker (black part) Bromo-PEG2-CH2-Boc (HY-141371) and Hty molecule (blue part) Adamantan-1-ylmethanamine (HY-W037848). The conjugate consisting of Hyt and linker parts is Adamantan-C-amide-PEG2-C-Br (HY-161974), and the activity control of the target protein ligand is Hydroxyl-ML-210 (HY-161973).
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