| DC50076 |
(S,R,S)-AHPC-Me-C3-NH2
Featured
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(S,R,S)-AHPC-Me-C3-NH2 is a novel PROTAC building block. |
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| DC50077 |
(S,R,S)-AHPC-Me-C4-NH2
Featured
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(S,R,S)-AHPC-Me-C4-NH2 is a novel PROTACA building block. |
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| DC50078 |
(S,R,S)-AHPC-Me-C8-NH2
Featured
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(S,R,S)-AHPC-Me-C8-NH2 is a novel PROTAC building block. |
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| DC50079 |
Thalidomide-O-amido-C5-NH2
Featured
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Thalidomide-O-amido-C5-NH2 is a novel PROTAC building block. |
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| DC70618 |
MS177
Featured
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MS 177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-1 g/kg) represses AML growth without apparent toxicity in PDX models. |
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| DC70620 |
MS934
Featured
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MS934 (MS-934) is a VHL-recruiting MEK1/2 degrader (PROTAC) with HT29 DC50 of 18/9 nM for MEK1/2 degradation, respectively.MS934 is more potent at inhibiting the growth of HT-29, SK-MEL-28, H3122, and SUDHL1 cells. MS934 also displays good plasma exposure in mice. |
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| DC70621 |
MS9715
Featured
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MS9715 (MS-9715) is a NSD3-targeting PROTAC designed by linking BI-9321, a NSD3 antagonist, which binds NSD3's PWWP1 domain, with an E3 ligase VHL ligand.MS9715 achieves effective and specific targeting of NSD3 and associated cMyc node in tumor cells.MS9715 effectively suppresses growth of NSD3-dependent hematological cancer cells.MS 9715 effectively suppresses NSD3-and cMyc-associated gene expression programs, resembling effects of the CRISPR-Cas9-mediated knockout of NSD3. |
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| DC70723 |
QC-01–175
Featured
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QC-01-175 is a hetero-bifunctional molecule designed to engage both tau and Cereblon (CRBN) to trigger tau ubiquitination and proteasomal degradation (tau PROTAC).QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal cell models, with minimal effect on tau from neurons of healthy controls.QC-01–175 also rescued stress vulnerability in FTD neurons, phenocopying CRISPR-mediated MAPT-knockout. |
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| DC70923 |
YX-2-107
Featured
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YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib. |
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| DC71088 |
MS5033 |
MS5033 is a potent PROTAC-based AKT (protein kinase B) degrader, with a DC50 of 430 nM in PC3 cells. |
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| DC71103 |
Pomalidomide-PEG4-COOH
Featured
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Pomalidomide-PEG4-COOH is a E3 ligase ligand-linker conjugate. Pomalidomide-PEG4-COOH contains the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology (extracted from patent WO2017184995A1). |
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| DC71142 |
Dimethyl-F-OICR-9429-COOH |
Dimethyl-F-OICR-9429-COOH a ligand for WD40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1 intermediate 19. Dimethyl-F-OICR-9429-COOH can be used in the synthesis of PROTACs. |
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| DC71174 |
PROTAC SOS1 degrader-1 |
PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 agonist with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity. |
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| DC71175 |
PROTAC TTK degrader-2 |
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells. |
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| DC71233 |
Azido-PEG2-VHL |
Azido-PEG2-VHL is a multikinase degrader which can be used in the synthesis of PROTACs. |
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| DC71237 |
SIAIS117 |
SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer. |
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| DC71244 |
YF135 |
YF135 is an efficient and reversible-covalent KRASG12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRASG12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway. |
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| DC71629 |
SS47 |
SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell treatment. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies. |
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| DC71630 |
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine |
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia. |
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| DC71631 |
dTAG-47 |
dTAG-47, heterobifunctional dTAG molecule, targets mutant FKBP12 (FKBP12F36V). FKBP12F36V serves as a degradation tag (dTAG) and is fused to a protein of interest. dTAG-47 can be used for the research of basal-like breast cancers (BBC). |
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| DC71632 |
PP-C8 |
PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC). |
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| DC71633 |
dTAG-47-NEG |
dTAG-47-NEG is an analog of dTAG-47 that cannot bind and recruit cereblon (CRBN). dTAG-47-NEG can be used as a heterobifunctional negative control of dTAG-47. |
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| DC71634 |
SIAIS164018 |
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, which is designed from Brigatinib, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib. |
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| DC71635 |
HD-TAC7 |
HD-TAC7 is a PROTAC HDAC3 degrader with a DC50 value of 0.32 μM. HD-TAC7 inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 3.6, 4.2, and 1.1 μM, respectively. HD-TAC7 can be used for the research of inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD). |
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| DC71636 |
MS9427 |
MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer. |
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| DC71678 |
(S,R,S)-AHPC-O-PEG1-propargyl |
(S,R,S)-AHPC-O-PEG1-propargyl (Compound 10b) is an E3 ligand for the synthesis of PROTAC. |
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| DC71924 |
DA-PROTAC |
DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research. |
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| DC71925 |
MS159 |
MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease. |
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| DC71926 |
MS9449 |
MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer. |
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| DC71927 |
XF067-68 |
XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5) (extracted from patent WO2019246570A1). |
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