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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
76 Results for "
PROTAC-based
" in MedChemExpress (MCE) Product Catalog:
Products (76)
76 Results for "PROTAC-based" in MCE Product Catalog:
30
30 Publications Verification
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ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively .
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4 Cited Publications
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KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .
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1 Cited Publications
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
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1 Cited Publications
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PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM .
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1 Cited Publications
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PROTAC RIPK degraders -2 is a non-peptide PROTAC based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes .
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1 Cited Publications
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PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 .
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1 Cited Publications
Cat. No.: HY-133120A
Purity: 99.27%
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
Cat. No.: HY-161157
CAS No.: 2451573-90-1
dTAG-13-NEG is a negative control of dTAG-13 (HY-114421). dTAG-13, a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 F36V with expression of FKBP12F36V in-frame with a protein of interest .
Cat. No.: HY-150251
CAS No.: 2497583-03-4
Synonyms: STAT3 degrader-2
SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a Ki of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506) .
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PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .
Cat. No.: HY-162412
CAS No.: 2841308-96-9
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PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .
Cat. No.: HY-173679
CAS No.: 2569517-30-0
RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD + site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC50=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections .
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia .
Cat. No.: HY-170859
CAS No.: 3110370-06-1
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AH078 is a PROTAC-based CK1δ/ε degrader (DC50=0.55 μM, Dmax=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma .
Cat. No.: HY-155218
CAS No.: 2488892-09-5
TMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC50 values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer .
Cat. No.: HY-160506
CAS No.: 2353493-69-1
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PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .
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PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) LIM Kinase (LIMK) ULK
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DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity .(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
