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 関連製品 (28)
関連製品 (28)
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MS1943
(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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LL-K8-22
0 ImagesLL-K8-22 is a dual degrader of CDK8 and cyclin C HyT, with DC50 values of 2.52 μM and 2.64 μM, respectively. LL-K8-22 inhibits phosphorylation of STAT1 Ser 727, phosphorylation of the C-terminal domain Ser 2/5 of RNA polymerase II, and phosphorylation of Rb. LL-K8-22 represses E2F- and MYC-driven transcriptional programs and exhibits antiproliferative effects. LL-K8-22 synchronously induces proteasome-dependent selective degradation of CDK8 and cyclin C without degrading CDK19, other CDK family members, or other cyclins. LL-K8-22 can be used in the research of triple-negative breast cancer and colon cancer.
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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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PCSK9 degrader 1
0 Images製品番号: HY-130245純度: 98.33%PCSK9 degrader 1 is a HyT-like PCSK9 degrader with a Ki of 107 nM. PCSK9 degrader 1 binds to the allosteric pocket between the catalytic domain and C-terminal domain of PCSK9. While maintaining key interactions with this protein, it extends the proteasome-recruiting moiety, thereby driving degradation via the proteasomal pathway. PCSK9 degrader 1 induces the degradation of both the precursor and mature forms of PCSK9, with DC50 values of 4.8 μM and 3.4 μM respectively, and does not significantly affect cell viability or the expression of housekeeping proteins. PCSK9 degrader 1 can be used in the research of coronary heart disease.
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(-)-Menthyloxyacetic acid
0 Images製品番号: HY-W093149CAS 番号: 40248-63-3
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TX2-121-1
0 Images製品番号: HY-118998CAS 番号: 1603845-42-6TX2-121-1 is a bifunctional hydrophobic tag Her3 degrader and also a Her3 inhibitor with an IC50 of 49 nM. TX2-121-1 covalently binds to Cys721 of Her3, induces Her3 degradation via the Hsp70/Hsp90-assisted proteasomal pathway, interferes with the heterodimerization of Her3 with Her2/c-Met, and attenuates downstream Erk/Akt signaling, thereby inhibiting Her3-dependent cancer cell growth. TX2-121-1 can be used for the research of non-small cell lung cancer, ovarian cancer and Her3-driven breast cancer.
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SKLB-0124
0 Images製品番号: HY-178114CAS 番号: 3065966-31-3SKLB-0124 is a selective PRMT6 degrader based on a hydrophobic labeling (HyT) method. SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer.
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LL-K9-3
0 ImagesLL-K9-3 is a selective CDK9-cyclin T1 HyT degrader, with DC50 values of 0.662 μM and 0.589 μM for CDK9 and Cyclin T1, respectively. LL-K9-3 lacks an E3 ligand moiety and induces polyubiquitination and proteasome-mediated synchronous degradation of CDK9 and cyclin T1 via a hydrophobic tag-mediated mechanism. LL-K9-3 downregulates the protein levels of androgen receptor (AR) and c-Myc, and exhibits antiproliferative and pro-apoptotic (apoptosis) activity in prostate cancer cells. LL-K9-3 can be used in studies related to prostate cancer.
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SARD279
0 Images製品番号: HY-164807CAS 番号: 1489236-55-6SARD279 is a HyT degrader of androgen receptor (AR). SARD279 binds to AR, recruits HSP70, mediates ubiquitin-dependent proteasomal degradation, and competitively inhibits the transactivation of AR. SARD279 exhibits antiproliferative activity in AR-dependent prostate cancer cells and castration-resistant prostate cancer cells, including those harboring the ARF876L mutation. SARD279 can be used in studies related to prostate cancer and castration-resistant prostate cancer.
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ALK degrader 4
0 Images製品番号: HY-182057CAS 番号: 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 Images製品番号: 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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BCR-ABL degrader 1
0 Images製品番号: HY-180798BCR-ABL degrader 1 is a hydrophobic tag degrader with GNF‑2 (HY-11007) as the ligand and Boc2His (HY-185595) as the hydrophobic tag. BCR-ABL degrader 1 mediates the degradation of BCR‑ABL with a DC50 of 19.9 μM. BCR-ABL degrader 1 induces the degradation of BCR-ABL fusion protein via the ubiquitin-proteasome pathway, a process involving Hsp70 and Hsp90. BCR-ABL degrader 1 downregulates p‑STAT5 and p‑SHP2, the downstream signaling molecules of BCR‑ABL. BCR-ABL degrader 1 can be used in the research of chronic myeloid leukemia.
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CDK9 degrader-1
0 Images製品番号: HY-176451CDK9 degrader-1 is a HyT-type CDK9 degrader that selectively induces protein degradation by recruiting ATG101 (with a DC50 of 0.4073 μM in HCT116 cells). CDK9 degrader-1 recruits ATG101 to initiate the autophagy-lysosome pathway, forming LC3-containing autophagosomes that fuse with lysosomes to degrade CDK9. CDK9 degrader-1 mediates the degradation of Cyclin T1 via the same autophagy-lysosome pathway. CDK9 degrader-1 induces downstream phenotypic effects associated with CDK9 degradation. CDK9 degrader-1 can be used in the research of colorectal cancer (Blue: hydrophobic group; Pnk: CDK9 ligand (HY-50940); Black: linker (HY-N0420)).
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(R,R)-PCSK9 degrader 1
0 Images製品番号: HY-130245ACAS 番号: 2216703-12-5(R,R)-PCSK9 degrader 1 is an isomer of PCSK9 degrader 1 (HY-130245). (R,R)-PCSK9 degrader 1 is a HyT-like PCSK9 degrader (IC50 of 655.4 nM) , and its PCSK9-binding site does not interfere with the binding of PCSK9 to LDL receptor. (R,R)-PCSK9 degrader 1 can be used in the research of atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, and related cardiovascular and cardiometabolic diseases.
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GPX4 degrader-1
0 Images製品番号: HY-181598CAS 番号: 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 Images製品番号: 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 Images製品番号: 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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Tubulin degrader 2
0 Images製品番号: HY-161641Tubulin degrader 2 is a tubulin HyT degrader and tubulin polymerization inhibitor, with a DC50 of 4.9 μM against α-tubulin in MCF-7 cells and an IC50 of 7.5 μM for the polymerization of purified recombinant tubulin. Tubulin degrader 2 binds to the colchicine-binding site of tubulin, induces proteasome-dependent degradation of α-tubulin and β-tubulin, inhibits the polymerization of purified recombinant tubulin, and triggers microtubule disruption and cell cycle arrest in cancer cells. Tubulin degrader 2 exhibits antitumor activity in a breast cancer allograft mouse model. Tubulin degrader 2 can be applied in the research of breast cancer, lung cancer, and colorectal cancer.
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