DC74470 |
SuO-Val-Cit-PAB-MMAE
Featured
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A drug-linker conjugate for antibody-drug conjugate by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide SuO-Val-Cit-PAB.. |
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DC74471 |
EN106 derivative 1 |
EN106 derivative 1 is a EN106 derivative used for PROTAC design, EN106 is a covalent ligand and recruiter for FEM1B E3 ligase for targeted protein degradation. |
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DC74472 |
EN106 derivative 2 |
EN106 derivative 2 is a EN106 derivative used for PROTAC design, EN106 is a covalent ligand and recruiter for FEM1B E3 ligase for targeted protein degradation. |
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DC74473 |
Thalidomide-O-PEG4-Acid |
Thalidomide-O-PEG4-Acid is a chemical linker for PROTAC design. |
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DC74474 |
(R)-SL18 |
(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM. |
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DC74475 |
ARD-1676 |
ARD-1676 (ARD1676) is a highly potent and orally efficacious PROTAC degrader of the androgen receptor (AR) with DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, respectively. |
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DC74476 |
BI 1810284 |
BI 1810284 (ACBI2, BI 01810284) is a potent, selective and orally bioavailable VHL-recruiting PROTAC degrader of SMARCA2 (DC50=1 nM in RKO cells), 30-fold selectivity over SMARCA4. |
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DC74477 |
BJG-05-039 |
BJG-05-039 is a PAK1-selective degrader consisting of NVS-PAK1-1 conjugated to lenalidomide, a recruiter of the E3 ubiquitin ligase substrate adaptor Cereblon. |
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DC74478 |
BSJ-04-146 |
BSJ-04-146 is a potent, selective FAK PROTAC (IC50=26 nM), induces potent and durable FAK degradation in pancreatic and breast cancer cell lines at 10 nM. |
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DC74479 |
BSJ-05-037
Featured
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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. |
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DC74480 |
BTX-6654 |
BTX-6654 is a potent, selective SOS1 cereblon-based bifunctional PROTAC degrader, reduces downstream signaling markers, pERK and pS6, and displayed antiproliferative activity in cells harboring various KRAS mutations. |
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DC74481 |
BWA-522 |
BWA-522 is a potent, orally bioavailable PROTAC degrader of the androgen receptor N-terminal domain (AR-NTD), induces AR-FL or AR-V7 protein degradationwith DC50 of 0.73 μM (AR-FL) and 0.67 μM (AR-V7) in VCaP cells. |
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DC74482 |
CC-3240 |
CC-3240 is a molecular glue degrader of CaMKK2 based on CC-8977 with bingding IC50 of 9 nM and DC50 of 100 nM (THP1 cells, Dmax=92%). |
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DC74483 |
Chk1 PROTAC-2 |
Chk1 PROTAC-2 is a potent Chk1 degrader with DC50 of 1.33 µM in A375 cells. |
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DC74484 |
CRBN(BRAF)-24 |
CRBN(BRAF)-24 is a potent small molecule degrader against oncogenic BRAF V600E protein, potently degrades BRAFV600E in a ubiquitin–proteasome system (UPS)-dependent manner and inhibits the proliferation of BRAFV600E-driven cancer cells. |
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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. |
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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. |
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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. |
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DC74488 |
DB0614 |
DB0614 is a CRBN-based PROTAC, induces the degradation of NEK9, FAK, CDK4, CDK6, and WEE1 in cells. |
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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. |
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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. |
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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. |
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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). |
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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. |
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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. |
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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%). |
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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. |
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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. |
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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). |
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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 |
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