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.
Alle PROTACs Isoform-spezifische Produkte anzeigen
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PROTACs Verwandte Produkte (1334)
Verwandte Produkte (1334)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC ERα Degrader-11
0 ImagesArt. -Nr.: HY-174870PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)).
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LUF7996
0 ImagesArt. -Nr.: HY-180571CAS. Nr.: 3104736-80-0LUF7996 is a CCR2 PROTAC Degrader degrading CCR2 with DC50 = 2.6 μM. LUF7996 demonstrates engagement of both and the E3 ligase cereblon and displays sustain and concentration-dependent degradation of CCR2. LUF7996 reliance on the lysosomal pathway to induce CCR2 degradation. LUF7996 efficiently inhibits monocyte migration in virto.
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PROTAC PI3K/110β degrader-2
0 ImagesArt. -Nr.: HY-174469CAS. Nr.: 3070438-79-5PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer.
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Tamoxifen-PEG-Clozapine
0 ImagesArt. -Nr.: HY-168869CAS. Nr.: 3104316-29-9Tamoxifen-PEG-Clozapine is a ERα PROTAC degrader. Tamoxifen-PEG-Clozapine induces ubiquitination and degradation of ERα protein. Tamoxifen-PEG-Clozapine mediates ERα degradation by utilizing UBR5 as a component of the ubiquitin-proteasome system. Tamoxifen-PEG-Clozapine exhibits anticancer activity against breast cancer. Tamoxifen-PEG-Clozapine can be used in the research of breast cancer.
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(S,R)-CFT8634
0 ImagesArt. -Nr.: HY-145925CCAS. Nr.: 2704617-95-6(S,R)-CFT8634 is a BRD9 PROTAC degrader that exerts activity via the ubiquitin-proteasome pathway. (S,R)-CFT8634 can be used in the research of acute myeloid leukemia, malignant rhabdoid tumor, synovial sarcoma, and multiple myeloma.
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PROTAC SMARCA2/4 degrader-33
0 ImagesArt. -Nr.: HY-162741CAS. Nr.: 2568276-36-6
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PROTAC TEAD/IAP degrader-1
0 ImagesArt. -Nr.: HY-181594PROTAC TEAD/IAP degrader-1 is a TEAD/IAP PROTAC degrader. PROTAC TEAD/IAP degrader-1 is also a specific and Nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPERs). PROTAC TEAD/IAP degrader-1 recruits cIAP1 to form ternary complexes, induces ubiquitination, proteasomal TEAD1, TEAD4 degradation. PROTAC TEAD/IAP degrader-1 inhibits TEAD transcriptional activity, reduces CTGF expression, and reduces cell proliferation. PROTAC TEAD/IAP degrader-1 can be used for the research of mesothelioma.
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PROTAC PAPD5 degrader 1
0 ImagesArt. -Nr.: HY-162327PROTAC PAPD5 degrader 1 is a selective PAPD5 PROTAC degrader. PROTAC PAPD5 degrader 1 induces ubiquitination and degradation of PAPD5 without causing degradation of PAPD7. PROTAC PAPD5 degrader 1 reduces Hepatitis B virus mRNA and Hepatitis B surface antigen levels in vitro. PROTAC PAPD5 degrader 1 inhibits both Hepatitis A virus and Hepatitis B virus. PROTAC PAPD5 degrader 1 can be used for research on Hepatitis A virus infection and Hepatitis B virus infection.
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Psa-AR
0 ImagesArt. -Nr.: HY-179056Psa-AR is a PROTAC degrader targeting PSMA, with a Kd of 7.2 nM. Psa-AR exhibits strong degradation capabilities for AR, AR-V7, and HSP90, and induces cell apoptosis. Psa-AR demonstrates potent tumor suppressive activity in the 22Rv1 xenograft tumor model. Psa-AR can be used in the research of castration-resistant prostate cancer.
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PROTAC SMARCA2 degrader-9
0 ImagesArt. -Nr.: HY-162746CAS. Nr.: 2568276-39-9
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RIP2 Kinase Inhibitor 4
0 ImagesArt. -Nr.: HY-136010CAS. Nr.: 2126803-41-4
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ML 2-23
0 ImagesArt. -Nr.: HY-153582ML 2-23 is a PROTAC degrader that recruits RNF114 to target BCR-ABL/c-ABL for degradation. ML 2-23 promotes proteasome-dependent degradation of the target protein and inhibits phosphorylation of downstream CRKL. At concentrations used for BCR-ABL degradation, ML 2-23 only causes slight impairment to the viability of cancer cells. ML 2-23 can be used in the research of chronic myeloid leukemia.
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PROTAC EML4-ALK Degrader-1
0 ImagesArt. -Nr.: HY-174368Synonyms: Pro-BAPROTAC EML4-ALK Degrader-2 (Pro-BA) is a selective and orally active linker-free EML4-ALK PROTAC degrader with the DC50 of 74 nM in H1322 cells (T1/2 = 8 h). PROTAC EML4-ALK Degrader-2 relies on GID4 and proteasome pathways to promote ubiquitination of target proteins, leading to cell apoptosis. PROTAC EML4-ALK Degrader-2 can be used for research on cancer.
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PROTAC BRD4 Degrader-34
0 ImagesArt. -Nr.: HY-174920CAS. Nr.: 1797406-70-2PROTAC BRD4 Degrader-34 (Compound MZ2) is a selective BRD4 PROTAC degrader (pDC50 = 8.4). PROTAC BRD4 Degrader-34 can induce BD2 degradation mediated by VHL. PROTAC BRD4 Degrader-34 can be used for research on cancer. (Pink: BRD4-BD2 Ligand (HY-78695); Blue: VHL Ligand (HY-125845); Black: Linker (HY-130524)).
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Arg-PEG1-Tαsyn
0 ImagesArt. -Nr.: HY-180976Arg-PEG1-Tαsyn is an α-syn PROTAC degrader with a DC50 of 0.28 μM in U251 cells. Arg-PEG1-Tαsyn employs the amino acid arginine (Arg) as the E3 ligase UBR1 ligand and a benzothiazole-aniline variant as the warhead for α-syn. Arg-PEG1-Tαsyn significantly reduces α-syn aggregates and improves the dopaminergic neuronal impairment and the locomotion with safety profile in vivo.Arg-PEG1-Tαsyn shows the high degradation effect in mammalian cells for both wild-type α-syn and the α-syn (A53T) mutant. Arg-PEG1-Tαsyn can be used for Parkinson’s disease research.
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PROTAC BTK Degrader-9
0 ImagesArt. -Nr.: HY-162280CAS. Nr.: 3034024-77-3PROTAC BTK Degrader-9 is a potent BTK PROTAC degrader with a DC50 of 1.29 nM (in Mino cells at 4 h). PROTAC BTK Degrader-9 induces the formation of a stable ternary complex with BTK and the CRBN E3 ubiquitin ligase, thereby mediating proteasomal degradation of BTK in a CRBN-dependent manner. PROTAC BTK Degrader-9 downregulates the RANKL-activated BTK-PLCγ2-Ca2+-NFATc1 signaling pathway. PROTAC BTK Degrader-9 alleviates alveolar bone resorption in periodontitis models of Mus musculus (house mouse). PROTAC BTK Degrader-9 can be used in research related to periodontitis.
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PROTAC CCR9 Degrader 1
0 ImagesArt. -Nr.: HY-181287PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a Ki value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease.
