DC74500 |
JET-209 |
JET-209 (JET209) is a potent, selective PROTAC degrader of CBP/p300 based on GNE-207 with DC50 of 0.05 nM for CBP and 0.2 nM for p300, Dmax >95% for both proteins in the RS4;11 leukemia cell line. |
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DC74501 |
JH-XII-03-02 |
JH-XII-03-02 is a highly potent, selective PROTAC degrader of LRRK2 with IC50 of 1 nM against both wt LRRK2 and LRRK2 G2019S. |
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DC74502 |
JWZ-1-80 |
JWZ-1-80 is a potent and selective PROTAC degrader of PI5P4Kγ with Kd of 510 nM, 1 uM induces 75% reduction of PI5P4Kγ in Molt4 cells. |
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DC74503 |
KH-103
Featured
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KH-103 is a highly potent, catalytically-driven glucocorticoid receptor (GR) PTORAC degrader, demonstrate excellent performance in passively preventing ligand-induced gene expression activation in the absence of partial agonistic transcriptional triggerin |
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DC74504 |
KYH1872 |
KYH1872 is a PROTAC that induces protein degradation via the KLHDC2 E3 ubiquitin ligase, KYH1872 is consisted of a C-terminal fragment of the SelK protein and promiscuous kinase inhibitor YHJ1039 via PGE linker. |
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DC74505 |
LL-K8-22 |
LL-K8-22 is a potent, selective dual degrader of of CDK8 and cyclin C (MDA-MB-468 cell DC50, 2.52 and 2.64 uM), significantly degrades CDK8 without reducing CDK19 and does not degrade other cyclin proteins. |
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DC74506 |
MS132 |
MS132 is a highly potent and selective VHL-recruiting WDR5 PROTAC degrader with DC50 of 92 nM in MIA PaCa-2 cells. |
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DC74507 |
MS147 |
MS147 (MS 147) is the first degrader of PRC1 core components, BMI1 and RING1B, comprises an EED small-molecule binder (EED226, Cat. PC-42321) linked to a ligand of the E3 ligase von Hippel-Lindau (VHL), degrades BMI1/RING1B in an EED-, VHL-, ubiquitinatio |
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DC74508 |
MS3227 |
MS3227 is a proteolysis-targeting chimera (PROTAC) that targets MDM2 by recruiting the E3 ligase VHL, resulting in proteasome-dependent degradation of MDM2. |
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DC74509 |
MTX-23 |
MTX-23 is a proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) splice variant-7 (AR-V7) and AR-full length (AR-FL) with DC50 of 0.37 and 2 uM, respectively. |
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DC74510 |
PIK5-12d |
PIK5-12d is a highly potent, selective, first-in-class PIKfyve PROTAC degrader, potently degrades PIKfyve protein with DC50 value of 1.48 nM and Dmax value of 97.7% in prostate cancer VCaP cells. |
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DC74511 |
PROTAC dCE-1 |
PROTAC dCE-1 is a potent, selective CBP/EP300 degrader targeting the histone acetyltransferase (HAT) domain, with DC50 value of 1.3 μM in LP1 cells. |
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DC74512 |
PTD10 |
PTD10 is a highly potent BTK PROTAC degrader with DC50 of 0.5 nM in TMD8 cells, inhibits cell growth and induces apoptosis more potently than parent molecule GDC-0853. |
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DC74513 |
QA-68-ZU81 |
QA-68-ZU81 (QA-68) is a EA-89-based BRD9 degrader that incorporates the EA-89 warhead into a cereblon (CRBN)-targeting proteolysis-targeting chimera (PROTAC). |
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DC74514 |
SelDeg51 |
SelDeg51 (Selective Degrader of FKBP51) is a potent, selective FKBP51 PROTAC with Kd of 18 nM, Emax=90%. |
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DC74515 |
TD-802 |
TD-802 is potent, cereblon-mediated androgen receptor PROTAC degrader, effectively inducs AR protein degradation with DC50 of 12.5 nM and Emax 93% in LNCaP prostate cancer cells. |
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DC74516 |
TMX-2172 |
TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively. |
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DC74517 |
TMX-4153 |
TMX-4153 (TMX4153) is a bivalent PIP4K2C degrader (MOLT4 cells, DC50=24 nM, Dmax=921% at 1 uM) based on TMX-4084, rapidly and selectively degrades endogenous PIP4K2C. |
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DC74518 |
U7D-1 |
U7D-1 is a selective USP7-degrading Proteolysis Targeting Chimera (PROTAC). U7D-1 showed selective and effective USP7 degradation, and maintained potent cell growth inhibition in p53 mutant cancer cells. |
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DC74519 |
UBX-382 |
UBX-382 (UBX382) is a potent and orally available proteolysis-targeting chimera (PROTAC) that induces potent BTK degradation in DLBCL cell line with DC50 of 4.5 nM. |
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DC74520 |
UNC7700 |
UNC7700 (UNC-7700) is a potent EED-targeted PRC2 degrader, contains a unique cis-cyclobutane linker and potently degrades all PRC2 components EED (DC50=111 nM; Dmax=84%), EZH2WT/EZH2Y641N (DC50=275 nM; Dmax=86%) and SUZ12 (Dmax=44%) in DLBCL cells. |
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DC74521 |
WD6305 |
WD6305 is a potent and selective proteolysis-targeting chimera (PROTAC) degrader of METTL3-METTL14 complex with DC50 of 140 nM (METTL3), Dmax of 91.9% in Mono-Mac-6 AML cell line. |
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DC74523 |
XY-07-35
Featured
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XY-07-35 is a potent, selective HDAC6 proteolysis targeting chimera (PROTAC) degrader with IC50 of 48.5 nM. |
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DC74524 |
YX968 |
YX968 is a potent, selecive HDAC3/8 dual PROTAC degrader with DC50 of 1.7 and 6.1 nM in degrading HDAC3 and HDAC8 respectively (MDA-MD-231 cell, 8 h). |
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DC74525 |
ZZ151 |
ZZ151 (ZZ-151) is a highly potent and selective SOS1 degrader PROTAC with DC50 of 15.7 nM (Dmax=100%). |
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DC74526 |
AdipoAI |
AdipoAI is a novel small molecule APN receptor (AdipoR, adiponectin receptor) agonist. |
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DC74527 |
ALY688 |
ALY688 (ADP 355) is an adiponectin mimetic adiponectin receptor (AdipoR) agonist, inhibits the growth of AdipoR1/AdipoR2-positive cancer cell lines (MCF-7 cell, 0.1-10 uM). |
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DC74528 |
K284
Featured
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K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals. |
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DC74529 |
Wyeth-1 |
Wyeth-1 (hAMCase inhibitor 1) is a potent, selective inhibitor of human acidic mammalian chitinase (hAMCase) with IC50 of 210 nM, 20-fold selectivity over hCHIT1. |
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DC74530 |
DL5050 |
DL5050 (DL 5050) is a potent selective agonist of human constitutive androstane receptor (CAR) with EC50 of 0.37 uM in cell-based luciferase reporter assays (Emax=3.8). |
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