| DC74448 |
SR-4133 |
SR-4133 (SR4133) is a potent and highly selective CK1ε isoform inhibitor with IC50 of 58 nM, no significant acitivity agianst CK1δ (IC50>10,000 nM). |
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| DC74449 |
BMD4702 |
BMD4702 is a small molecule Dishevelled (Dvl) PDZ domain with binding Kd of 186 nM. |
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| DC74450 |
BMD4722 |
BMD4722 is a highly potent, small-molecule inhibitor of Dvl-CXXC5 interaction with IC50 of 2.59 uM, directly binds to the Dvl PDZ domain (Kd=22.3 uM). |
|
| DC74451 |
NPL-4011 |
NPL-4011 is a specific small molecule inhibitor of PDZ domain of human Dvl1 (Dvl1-PDZ) with KD vaule of 34.5 uM in NMR titration experiments. |
|
| DC74452 |
MDB5 |
MDB5 is a potent hedgehog (Hh) signaling pathway inhibitor, exhibits stronger inhibition of the Hh pathway and anticancer effect in vitro and vivo than GDC-0449. |
|
| DC74453 |
Picoberin |
Picoberin is a highly potent (low picomolar) inhibitor of purmorphamine- and Sonic Hedgehog (Shh)-induced osteogenesis with IC50 of 3 pM, acts as an AhR agonist and induces the expression of AhR target genes, thereby suppressing osteoblast differentiation |
|
| DC74454 |
aNDR1
Featured
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aNDR1 (NDR1 agonist) is a specific small-molecule agonist of Nuclear Dbf2-related kinase 1 (NDR1, STK38), specifically inhibits CRPC cells and promotes kinase activity of NDR1. |
|
| DC74455 |
TRULI |
TRULI is a small molecule Yap signaling activator, acts as an ATP-competitive inhibitor of Lats kinases in vitro (Lats1 kinase, IC50=0.2 nM, 10 uM ATP), prevents Yap phosphorylation in the cell-based assays with EC50 of 510 nM. |
|
| DC74456 |
UNC-BE4-017 |
UNC-BE4-017 is a selective STK3 small-molecule inhibitor, also potently inhibits JAK1, JAK2, and JAK3, but not other kinases in a panel of 48 kinases. |
|
| DC74457 |
UNC-SOB-5-16 |
UNC-SOB-5-16 is a potent, selective STK3 small-molecule inhibitor with IC50 of 22 nM, also inhibits LRRK2. |
|
| DC74458 |
AG-1031 |
AG-1031 (AG1031) is a specific small molecule inhibitor of the double-stranded DNA binding activity of positive coactivator 4 (PC4) with IC50 of 2.5 uM, more effectively than its single-stranded DNA binding activity (IC50=15 uM). |
|
| DC74459 |
Z271-0326
Featured
|
Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC). |
|
| DC74460 |
MRT-92 |
MRT-92 is a potent selective Smoothened (Smo) receptor antagonist (Kd=0.3 nM), inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation with IC50 of 0.4 nM. |
|
| DC74461 |
INS018_055 |
INS018_055 (INS018-055) a selective small-molecule TRAF2- and NCK-interacting kinase (TNIK) inhibitor with Kd value of 4.32 nM and IC50 of 31 nM, inhibits TGF-β-induced α-SMA protein expression in MRC-5 cells with IC50 of 27.14 nM. |
|
| DC74462 |
C644-0303 |
C644-0303 is a novel Wnt/β-catenin signaling inhibitor (IC50=4.2 uM) with antitumor efficacy, inhibits both constitutive and ligand activated Wnt signals and its downstream gene expression. |
|
| DC74463 |
ISQ-1 |
ISQ-1 is a potent in vitro inhibitor of several cancer cell lines (LS174T cell proliferation, IC50=100 nM), inhibits Wnt signaling and also activates adenosine monophosphate kinase (AMPK). |
|
| DC74464 |
LPD-01 |
LPD-01 is a small molecule inhibitor of the Wnt/β-catenin signaling pathway, directly binds to importin7, inhibits the transactivation of target genes of the Wnt/β-catenin signaling pathway. |
|
| DC74465 |
WNTinib |
WNTinib is a multi-kinase inhibitor with specificity against β-catenin (CTNNB1) mutant hepatocellular carcinoma, harnesses the KIT/MAPK/EZH2 pathway, shows durable and selective transcriptional repression of mutant β-catenin/Wnt targets through nuclear tr |
|
| DC74466 |
AMG2008827 |
A potent, selective γ-secretase inhibitor that significantly reduces the right ventricular systolic pressure and right heart hypertrophy in hypoxia/SU5416 (SUHx) rats.. |
|
| DC74467 |
RXC004
Featured
|
RXC004 (RXC-004) is a potent, selective Porcupine (PRCN) inhibitor, inhibits functional Wnt production from mouse L-Wnt3a cells with IC50 of 64 pM in luciferase reporters assays. |
|
| DC74468 |
WHN-88 |
WHN-88 is a potent, selective Porcupine (PORCN) inhibitor, inhibits Wnt/β-catenin signaling with IC50 of ST-Luc of 0.02 uM. |
|
| DC74469 |
ZD06519 |
ZD06519 is a novel camptothecin payload for antibody drug conjugates (ADCs) with highp ayload potency (~1 nM). |
|
| DC74470 |
SuO-Val-Cit-PAB-MMAE
Featured
|
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.. |
|
| 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. |
|
| 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. |
|
| DC74473 |
Thalidomide-O-PEG4-Acid |
Thalidomide-O-PEG4-Acid is a chemical linker for PROTAC design. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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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