PROTACs

25 products · Page 1 of 1

All small molecule research tools

DC7042

GSK-126

GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.

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DC7150

Birabresib (OTX015)

Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.

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DC5147

Molibresib(I-BET-762）

GSK 525762A is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.

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DC5019

(+)-JQ1

(+)-JQ-1 is a BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)).

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DC8261

(-)-JQ-1

(-)-JQ-1 is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (−)-JQ1 has no effect.

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DC5183

I-BET151

I-BET151 is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.

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DC8468

Ceralasertib (AZD6738)

AZD6738 is a potent inhibitor of ATR kinase with an IC50 of 1 nM.

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DC7143

GSK-343

GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.

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DC21360

MZ1

MZ 1 is a BRD4 protein degrader based on PROTAC technology.

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DC70923

YX-2-107

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…

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DC12022

dBET6

dBET6 is a highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.

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DC55003

XY028-140 (MS140)

XY028-140 (MS140) is a potent and selective PROTAC-based CDK4/CDK6 kinase degrader. XY028-140 specifically inhibits RB-E2F signaling and reduces CDK4 and CDK6 protein levels in a dose- and time-dependent manner in…

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DC48369

AGB1

AGB1 is a fast, highly selective, and potent bump-and-hole (B&H)-PROTAC degrader for BromoTag. AGB1 exhibits degradation for Ab:Brd4BD2 L387A and Ab: BromoTag-Brd2 with pDC50s of 7.8 and 7.9. AGB1 exhibits binary…

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DC60559

PT-179

PT-179 is a new orthogonal immunomodulatory drug (IMiD) derivative that binds CRBN but does not induce degradation of off-target proteins. PT-179 potently degrades proteins fused to SD40 at either the N or C terminus.

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DC11387

Erdafitinib

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

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DC10656

(+)-JQ1 carboxylic acid

JQ-1 carboxylic acid is a highly potent, selective and cell-permeable BRD4 inhibitor with IC50s of 77 nM and 33 nM for BRD4(1) and BRD4(2), respectively.

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DC11579

VH032

VH-032 (VHL ligand 1) is a VHL ligand for PROTAC and potent, small molecule inhibitor of the VHL/HIF-1α interaction with Kd of 185 nM.

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DC65801

ARV-102

ARV-102 is a highly potent, orally bioavailable PROTAC that targets LRRK2 with a of 0.14 nM, designed to cross the blood-brain barrier to address neurodegenerative diseases. By hijacking the body’s ubiquitin-proteasome…

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DC70723

QC-01–175

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…

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DC21351

MS4078

MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19 nM for binding affinity to ALK[1].

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DC70618

MS177

MS177 (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…

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DC74479

Autotaxin-IN-8

BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78. BSJ-05-037 induces potent degradation of ITK dependent on CRBN, neddylation, and the…

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DC22335

E3 ligase Ligand 1A ((S,R,S)-AHPC-Me)

E3 ligase Ligand 1A is a ligand of E3 ligase, used in PROTAC technology; E3 ligase Ligand 1A can be used in the research of cancer.

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DC26119

VHL ligand 2 hydrochloride ((S,R,S)-AHPC-Me hydrochloride)

VHL ligand 2 hydrochloride is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology.

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DC12024

ARV-825

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient…

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