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
All Product Categories
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PROTACs Related Products (1358)
Related Products (1358)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC SKP2 Degrader-1
0 ImagesPROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research.
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PROTAC STING degrader-4
0 ImagesCat. No.: HY-176180Purity: 98.96%PROTAC STING degrader-4 is a nitro-free covalent STING PROTAC degrader with a DC50 of 3.23 μM. PROTAC STING degrader-4 effectively inhibits STING as well as its downstream signaling, such as p-TBK1 and p-NF-κB (p-P65), and immune-inflammatory cytokines. PROTAC STING degrader-4 mitigates kidney and blood inflammation in Cisplatin (HY-17394)-induced acute kidney injury (AKI) mice model.
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PROTAC ERα Degrader-6
0 ImagesCat. No.: HY-157765CAS No.: 3065420-66-5
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YN14
0 ImagesCat. No.: HY-155356Purity: 99.08%YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
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dWIZ-1
0 ImagesCat. No.: HY-159098dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease.
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PP-C8
0 ImagesPP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC).
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AZD9750
0 ImagesAZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant ARL702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research.
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PROTAC K-Ras Degrader-5
0 ImagesCat. No.: HY-168669CAS No.: 3052745-16-8PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC50 of <100 nM for KRASG12D. PROTAC K-Ras Degrader-5 recruits KRASG12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses pERK levels downstream of KRASG12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer.
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dBRD4-BD1
0 ImagesdBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1.
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LD-110 trihydrochloride
0 ImagesCat. No.: HY-178825BLD-110 trihydrochloride is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 trihydrochloride promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 trihydrochloride inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 trihydrochloride can be used for the study of esophagus squamous cancer.
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PROTAC SOS1 degrader-1 TFA
0 ImagesCat. No.: HY-145737APurity: 98.38%PROTAC SOS1 degrader-1 TFA is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd value of 44 nM. PROTAC SOS1 degrader-1 TFA induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 TFA reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 TFA inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 TFA can be used for the research of KRAS-driven cancers.
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LZ-07
0 ImagesCat. No.: HY-172590Purity: 98.27%LZ-07 is a IRAK4 PROTAC degrader (DC50 = 1.14 nM). LZ-07 leads to marked suppression of cytokines including IL-6, IL-1β, TNF-α, and IL-10 upon degradation of IRAK4. LZ-07 can be studied in research for autoimmune diseases (Pink: IRAK4 ligand (HY-172591); Blue: CRBN ligand (HY-34590); Black: linker (HY-B0149); CRBN ligand + linker: HY-172593).
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MI-389
0 ImagesMI-389 is a potent menin-MLL interaction inhibitor (IC50=25 nM) and a CRBN-recruiting, GSPT1-targeted PROTAC degrader. MI-389 upregulates myeloid differentiation-related genes that are lowly expressed in primitive hematopoietic progenitor cells, thereby inducing myeloid differentiation phenotypic changes in MLL-rearranged leukemia cells. MI-389 competitively blocks the MG-H1-RAGE interaction to interfere with the AGEs-RAGE pathway, thus alleviating AGEs-induced HUVEC injury. MI-389 can be used in studies related to MLL-rearranged acute leukemia.
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Homo-BacPROTAC7 TFA
0 ImagesCat. No.: HY-153572AHomo-BacPROTAC7 TFA is a PROTAC protein degrader targeting ClpC1/ClpC2 with a Kd of 0.5-2.5 nM for both targets. Homo-BacPROTAC7 (TFA) acts as a bactericidal agent, induces killing of pathogenic mycobacteria, retains activity against dormant-like mycobacterial cells with reduced intracellular ATP levels, and shows elevated antibiotic potency relative to its parent monomer. Homo-BacPROTAC7 (TFA) can be used for the research of tuberculosis.
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GNE-987 GSH linker-2
0 ImagesCat. No.: HY-138634Purity: 99.48%GNE-987 GSH linker-2 is a drug-linker conjugates for ADC. GNE-987 GSH linker-2 is a conjugation of PROTAC GNE-987 (HY-129937A) and ADC linker GSH linker-2 (HY-182740), and can be used to prepare antibody-drug conjugates (ADC) for BRD4 degradation. GNE-987 GSH linker-2 can be used for the research of cancer.
