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
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PROTACs Related Products (1334)
Related Products (1334)
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Antibodies (1)
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PROTACs Isoform Comparison
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QZ2135
0 ImagesCat. No.: HY-170852QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854).
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PROTAC BRD4 Degrader-48
0 ImagesCat. No.: HY-184923PROTAC BRD4 Degrader-48 is a BRD4 degrader with a Kd of 0.69 μM for human BRD4 and a DC50 of 0.21 μM. PROTAC BRD4 Degrader-48 binds to BRD4 and GID4 to form a ternary complex, and induces ubiquitination and degradation of BRD4 via the ubiquitin-proteasome pathway. PROTAC BRD4 Degrader-48 inhibits proliferation and migration of tumor cells, blocks tumor growth, and maintains degrading activity even in VHL- and CRBN-deficient models. PROTAC BRD4 Degrader-48 can be used in studies related to renal cell carcinoma.
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PROTAC SMARCA2/4 degrader-36
0 ImagesCat. No.: HY-170347CAS No.: 3033588-00-7
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PROTAC IRAK4 degrader-12
0 ImagesCat. No.: HY-168586CAS No.: 2919995-09-6PROTAC IRAK4 degrader-12 is an orally active IRAK4 PROTAC degrader with a DC50 of 4.87 nM in K562 IRAK4-HiBiT cells. PROTAC IRAK4 degrader-12 induces protein degradation of IRAK4, IKZF1 and IKZF3. It inhibits the proliferation of diffuse large B-cell lymphoma cells. It suppresses tumor growth in mouse xenograft models of lymphoma cells. PROTAC IRAK4 degrader-12 can be used for the research of B-cell lymphoma and diffuse large B-cell lymphoma.
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ERD-12310A
0 ImagesCat. No.: HY-164924CAS No.: 3026007-23-5ERD-12310A is an orally active ERα PROTAC degrader, with a Ki value of 0.95 nM against human ERα and a DC50 of 47 pM for ERα in MCF-7 cells. ERD-12310A forms a ternary complex with ERα and the CRBN E3 ubiquitin ligase, thereby inducing ubiquitination and proteasomal degradation of wild-type and ESR1Y537S mutant ERα. ERD-12310A induces tumor regression in ER+ breast cancer xenografts and inhibits tumor growth in ESR1Y537S mutant breast cancer xenografts. ERD-12310A can be used in studies related to ER-positive breast cancer and ESR1-mutant breast cancer.
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PROTAC CBP/p300/BRD4 Degrader-1
0 ImagesCat. No.: HY-181758CAS No.: 3109024-12-3PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer.
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PROTAC ATR degrader-4
0 ImagesCat. No.: HY-184293PROTAC ATR degrader-4 is a PROTAC-based ATR kinase degrader, with a DC50 of 6.18 μM and a Dmax of 71.42% in LoVo cells. PROTAC ATR degrader-4 downregulates ATR protein expression, inducing nuclear envelope rupture, genomic instability, DNA damage and apoptosis. PROTAC ATR degrader-4 exhibits anti-tumor activity in xenograft tumor mouse models and can be used for the research of atm-deficient cancers.
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PROTAC Tubulin degrader-2
0 ImagesCat. No.: HY-181143PROTAC Tubulin degrader-2 is a cereblon (CRBN)-dependent α/β-tubulin PROTAC degrader with DC50 values of 1.73 μM and 1.38 μM. PROTAC Tubulin degrader-2 can inhibit cancer cells proliferation and migration. PROTAC Tubulin degrader-2 can induce G2/M arrest, apoptosis, ROS accumulation. PROTAC Tubulin degrader-2 can be used for the research of cancer, such as non-small-cell lung cancer.
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PROTAC FLT3/CDK9 degrader-1
0 ImagesCat. No.: HY-148521CAS No.: 3033084-05-5
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PROTAC EZH2 Degrader-17
0 ImagesCat. No.: HY-181300CAS No.: 3093642-23-7
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PROTAC TEAD1/IAP degrader-1
0 ImagesCat. No.: HY-181534PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma.
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PROTAC SMARCA2/4 degrader-17
0 ImagesCat. No.: HY-163870CAS No.: 2568276-88-8PROTAC SMARCA2/4-degrader-17 (Compound I-345) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-17 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM.
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PROTAC SMARCA2/4 degrader-25
0 ImagesCat. No.: HY-162813PROTAC SMARCA2/4 degrader-25 is a selective SMARCA2/SMARCA4 PROTAC degrader with selective anti-tumor activity. PROTAC SMARCA2/4 degrader-25 is activated by endogenous GSH, forms a ternary complex with SMARCA2 or SMARCA4 and VHL E3 ubiquitin ligase, and mediates degradation via the proteasome pathway. PROTAC SMARCA2/4 degrader-25 induces DNA damage and apoptosis, and inhibits cancer cell proliferation. PROTAC SMARCA2/4 degrader-25 is applicable to lung cancer-related research.
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PROTAC Akt3 Degrader-1
0 ImagesCat. No.: HY-175975CAS No.: 3048204-93-6
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PROTAC FGFR3 Degrader-1
0 ImagesCat. No.: HY-181153PROTAC FGFR3 Degrader-1 is a fibroblast growth factor receptor 3 (FGFR3) PROTAC degrader, promotes FGFR3 degradation via the ubiquitin-proteasome pathway, and inhibits the downstream FGFR3/PI3K/AKT signaling pathway. PROTAC FGFR3 Degrader-1 can be used for the research of hepatocellular carcinoma.
