| DC74485 |
CRBN(FLT3)-8 |
CRBN(FLT3)-8 a highly potent FLT3 degrader by introducing gilteritinib into targeted protein degradation technology, potently degrades FLT3-ITD via UPS and inhibits the proliferation of FLT3-ITD mutant AML cells more effectively than gilteritinib. |
|
| DC74486 |
DAS-5-oCRBN |
DAS-5-oCRBN is a potent and selective PROTAC for c-Src kinase with DC50 value of 3 nM, without effect on Bcr-Abl. |
|
| DC74487 |
DAS-CHO-5-oCRBN |
DAS-CHO-5-oCRBN is a potent and selective PROTAC for c-Src kinase with DC50 value of 62 nM in CAL148 cells. |
|
| DC74488 |
DB0614 |
DB0614 is a CRBN-based PROTAC, induces the degradation of NEK9, FAK, CDK4, CDK6, and WEE1 in cells. |
|
| DC74489 |
DBt-10 |
DBt-10 is a potent BTK-specific DCAF1 PROTAC with TR-FRET IC50 of 136 nM, potently degrades BTK with DC50 of 137 nM in TMD8 BTK-GFP/mCherry cell-based assays. |
|
| DC74490 |
dEALK1 |
dEALK1 is a small-molecule degrader of EML4-ALK fusion proteins with binding constant (Kd) value of 44 nM for kinase domain of recombinant ALK, overcomes resistance to ALK inhibitor ceritinib. |
|
| DC74491 |
DeFer-2 |
DeFer-2 is an oleic acid (OA)-based ferritin-targeting PROTAC binding Kd of 17.1 uM, degrades ferritin and rapidly elevates the free iron content, induces pyroptosis. |
|
| DC74492 |
Degradomer D-1 |
Degradomer D-1 is a selective proteasomal degrader of IRAK3 with Kd of 100 nM, DC50 of 94 nM, displays no binding affinity against IRAK4 (Ki >10 uM). |
|
| DC74493 |
DU-14 |
DU-14 is a highly potent and selective small molecule degrader for both PTP1B and TC-PTP with DC50 values of 4.3 and 4.8 nM, respectively, in HEK293 cells after 16 hours treatment. |
|
| DC74494 |
GNE-0011 |
GNE-0011 is a monovalent, JQ1-based BRD4 degrader that is not linked to an E3 ligase binder, triggers proteasomal and ubiquitin-dependent selective degradation of BRD4 over BRD2 and BRD3. |
|
| DC74495 |
HDAC3 PROTAC P7 |
HDAC3 PROTAC P7 is a potent and selective HDAC3-directed PROTAC with IC50 of 40 nM (HDAC3 deacetylase activity), effectively induces HDAC3 degradation with DC50 of 0.6 nM in THP-1 cells (Emax=90%). |
|
| DC74496 |
HJM-561 |
HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively. |
|
| DC74497 |
HPP-9 |
HPP-9 is a potent BET bromodomain degrader that acts through a PROTAC mechanism, HPP-9 is a long-acting Hedgehog pathway inhibitor. |
|
| DC74498 |
INY-06-061 |
INY-06-061 is a potent and selective heterobifunctional degrader of ERK5 with binding Kd of 12 nM and DC50 of 21 nM in MOLT4 cells (5h treatment). |
|
| DC74499 |
JCS-1 |
JCS-1 is a RG3039-based degarder (PROTAC) of the RNA decapping scavenger protein DcpS exhibiting effective degradation of DcpS at nanomolar concentrations, non-covalently binds DcpS and recruits the E3 ligase VHL, induces potent, rapid, and sustained DcpS |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC74503 |
KH-103
Featured
|
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 |
|
| 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. |
|
| 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. |
|
| DC74506 |
MS132 |
MS132 is a highly potent and selective VHL-recruiting WDR5 PROTAC degrader with DC50 of 92 nM in MIA PaCa-2 cells. |
|
| 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 |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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). |
|
| DC74514 |
SelDeg51 |
SelDeg51 (Selective Degrader of FKBP51) is a potent, selective FKBP51 PROTAC with Kd of 18 nM, Emax=90%. |
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