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 (1355)
Related Products (1355)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC PAPD5 degrader 1
0 ImagesCat. No.: 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 ImagesCat. No.: 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 ImagesCat. No.: HY-162746CAS No.: 2568276-39-9
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RIP2 Kinase Inhibitor 4
0 ImagesCat. No.: HY-136010CAS No.: 2126803-41-4
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ML 2-23
0 ImagesCat. No.: 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 ImagesCat. No.: 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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Arg-PEG1-Tαsyn
0 ImagesCat. No.: 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 ImagesCat. No.: HY-162280CAS No.: 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 ImagesCat. No.: 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.
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Phe-PEG1-Dasa
0 ImagesCat. No.: HY-180962CAS No.: 3037776-73-8Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, with its DC50 being 1.56 nM. Phe-PEG1-Dasa uses a single amino acid (Phe) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, thus being called a mini-PROTAC. Phe-PEG1-Dasa significantly inhibits the proliferation of K562 cells. Phe-PEG1-Dasa can be used for the study of leukemia.
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JPS014
0 ImagesCat. No.: HY-145815CAS No.: 2669785-76-4JPS014 is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3, with DC50 values of 0.91 μM, 4.19 μM and 0.64 μM, respectively. JPS014 recruits the VHL E3 ligase to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS014 acts as a submicromolar inhibitor of the HDAC1-CoREST, HDAC2-CoREST and HDAC3-SMRT complexes in vitro. JPS014 increases the level of H3K56ac, reduces the stability of LSD1 and SIN3A, and induces cell apoptosis (apoptosis). JPS014 can be used for the research of colon cancer.
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RD-23
0 ImagesCat. No.: HY-168867CAS No.: 3053537-06-4RD-23 is an orally active and selective RET PROTAC degrader, with DC50 values of 5.6 nM and 11.7 nM against RETWT and RETG810C mutants, respectively. RD-23 inhibits purified RET kinase activity with an IC50 of 0.371 nM. RD-23 suppresses the activation of downstream Shc signaling and induces apoptosis. RD-23 can be used for the research of RET-related cancers.
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dCE-2
0 ImagesCat. No.: HY-161958dCE-2 is a CBP/EP300 PROTAC degrader with a DC50 of 40 nM against CBP. dCE-2 forms a ternary complex with the bromodomains of CBP/EP300 and the CRBN E3 ligase, driving proteasomal degradation of CBP/EP300 via positive cooperativity. dCE-2 is applicable to research related to multiple myeloma, prostate cancer, and neuroblastoma.
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PROTAC BTK Degrader-13
0 ImagesCat. No.: HY-168963PROTAC BTK Degrader-13 is a reagent targeting BTK, with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 degrades BTK in a proteasome-dependent manner and inhibits BTK-mediated downstream signaling pathways by reducing the phosphorylation levels of BTK and p38 MAPK. PROTAC BTK Degrader-13 exerts selective cytotoxic effects on BTK-overexpressing lymphoma cells and ITK-positive cells. PROTAC BTK Degrader-13 can be used in studies related to B-cell lymphoma.
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YN14 (mixture of diastereomers)
0 ImagesCat. No.: HY-155356ACAS No.: 3053689-54-3YN14 mixture of diastereomers is the diastereomers of YN14 (HY-155356). 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.
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PROTAC FLT3/CHK1 Degrader-1
0 ImagesCat. No.: HY-178858PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML).
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PROTAC BET Degrader-18
0 ImagesCat. No.: HY-184335CAS No.: 3097564-20-7PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis, while suppressing oncoprotein expression. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer.
