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 (1323)
Related Products (1323)
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Antibodies (1)
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PROTACs Isoform Comparison
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Cath-L-dBET1
0 ImagesCat. No.: HY-173257Cath-L-dBET1 is a PROTAC degrader targeting BRD4. Cath-L-dBET1 has an IC50 value of 2.8 μM in MDA-MB-231 cells. Cath-L-dBET1 can be activated by cathepsin L (Cath-L) and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.
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BRD4 degrader-6
0 ImagesCat. No.: HY-173327CAS No.: 3055207-38-7BRD4 degrader-6 is a dimeric BDR4 PROTAC degrader (DC50: < 0.1 μM). BRD4 degrader-6 promotes the ubiquitination and degradation of BDR4 and has anticancer activity.
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Scopadulciol
0 ImagesCat. No.: HY-183390CAS No.: 136565-26-9Scopadulciol is an orally effective β-catenin degrader, HSV-TK activator and proton pump inhibitor. By inducing β-catenin degradation, Scopadulciol downregulates the expression of downstream target genes such as cyclin D1, c-myc, and survivin; it also upregulates DR4/DR5 and downregulates Bcl-2, thereby exerting cytotoxicity and inducing apoptosis in cancer cells. Scopadulciol enhances the tumor-killing and bystander effects of prodrugs via activating HSV-TK, and can inactivate HSV-1. It shows synergistic antiviral effects when combined with Acyclovir (HY-17422) or Ganciclovir (HY-13637), with no cytotoxicity as a single agent. Scopadulciol can be applied in research related to bladder cancer, cervical cancer, glioblastoma, and digestive system cancers.
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PROTAC HDAC8 Degrader-4
0 ImagesCat. No.: HY-181024PROTAC HDAC8 Degrader-3 (Compound BP6) is an efficient, selective and low-toxicity HDAC8 PROTAC degrader with a DC50 of 80 nM. PROTAC HDAC8 Degrader-3 exhibits IC50 of PROTAC for HDAC8 and CRBN of 0.26 and 30 μM respectively. PROTAC HDAC8 Degrader-3 increases the level of Ac-SMC3, stabilizes p53 and sensitizes targeted reagents (such as Idasanutlin (HY-15676)), demonstrating its great potential in combination therapy.
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PROTAC SMARCA2 degrader-16
0 ImagesCat. No.: HY-162742CAS No.: 2568276-37-7
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PROTAC sEH degrader-3
0 ImagesCat. No.: HY-175392CAS No.: 3093413-94-3PROTAC sEH degrader-3 (Compound 1a) is a targeted sEH PROTAC degrader that can selectively degrade sEH in the cytosol without affecting sEH in peroxisomes. PROTAC sEH degrader-3 degrades sEH through a CRBN-dependent lysosomal pathway rather than the proteasome, with an IC50 of 0.8 nM against hsEH. PROTAC sEH degrader-3 can inhibit endoplasmic reticulum stress and can be used in the research of inflammation, metabolic diseases, and other diseases related to endoplasmic reticulum stress.
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PROTAC SMARCA2/4 degrader-6
0 ImagesCat. No.: HY-159457CAS No.: 2568277-87-0
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MS99-β-Gal
0 ImagesCat. No.: HY-177945CAS No.: 3055593-63-7Synonyms: Gal-MS99MS99-β-Gal (Gal-MS99) is a galactose-modified NPM-ALK PROTAC degrader. MS99-β-Gal is only hydrolyzed by SA-β-gal and esterase in senescent cancer cells, releasing MS99, which specifically degrades the NPM-ALK fusion protein. MS99-β-Gal shows an IC50 of 454.8 nM for aging Karpas 299 cells, significantly lower than that of normal Karpas 299 cells (IC50 = 2.162 μM). MS99-β-Gal can be used for the research of cancer.
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PROTAC PIN1 degrader-2
0 ImagesCat. No.: HY-186218CAS No.: 3083422-10-7PROTAC PIN1 degrader-2 is a PROTAC PIN1 degrader. PROTAC PIN1 degrader-2 reduces PIN1-mediated oncogene expression, upregulates PIN1-inhibited tumor suppressor genes, and exerts killing effects on cancer cells. PROTAC PIN1 degrader-2 inhibits tumor growth in breast cancer mouse xenograft models. PROTAC PIN1 degrader-2 can be used for the research of breast cancer.
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SJH1-51B
0 ImagesCat. No.: HY-162240SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research.
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dIRF4-2
0 ImagesCat. No.: HY-185697dIRF4-2 is a selective IRF4 PROTAC degrader with a DC50 value of 2.2 μM. dIRF4-2 forms a ternary complex between IRF4 and CRBN, inducing ubiquitination and proteasomal degradation of IRF4. dIRF4-2 downregulates MYC. dIRF4-2 exhibits anticancer activity against myeloma. dIRF4-2 acts as a chemical probe for investigating IRF4 function, mimicking the IRF4 gene knockout phenotype. dIRF4-2 can be used in the research of multiple myeloma.
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PROTAC SOS1 degrader-5
0 ImagesCat. No.: HY-161173CAS No.: 2836273-61-9PROTAC SOS1 degrader-5 is a potent SOS1 PROTAC degrader with a DC50 value of 13 nM. PROTAC SOS1 degrader-5 induces CRBN-dependent ubiquitination and degradation of SOS1 protein, inhibits the proliferation of KRASG12C-mutated cancer cells, and suppresses tumor growth in xenograft models. PROTAC SOS1 degrader-5 can be used in studies related to KRASG12C-mutated non-small cell lung cancer.
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PROTAC BRD2/BRD4 degrader-1
0 ImagesCat. No.: HY-130612CAS No.: 2570470-42-5PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect.
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SK5527
0 ImagesCat. No.: HY-179641SK5527 is a selective AURKA PROTAC degrader degrading AURKA with DC50 = 2 nM. SK5527 bind to NanoLuc-AURKA with an IC50 of 20 nM. SK5527 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK5527 efficiently reduced AURKA levels in vivo. SK5527 can be used for neuroblasto2ma research.
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PROTAC FAK degrader 3
0 ImagesCat. No.: HY-175459PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). PROTAC FAK degrader 3 induces FAK degradation dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers.
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PROTAC SMARCA2 degrader-36
0 ImagesCat. No.: HY-181909PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers.
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PROTAC BRD4 Degrader-33
0 ImagesCat. No.: HY-174811PROTAC BRD4 Degrader-33 is an enzyme activated clickable BRD4 PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model.
