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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC73150 MR-2088
MR-2088 is a potent and selective ULK1/2 inhibitor with IC50 of 2.0 nM and MST Kd value of 1.5-4.4 nM (ULK1), efficiently inhibits autophagy.
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DC73149 SK-124
SK-124 (SK124) is a potent, selective, orally active SIK2/SIK3 inhibitor with IC50 of 8.8/11.3 nM in cell-based NanoBRET assays, 15-fold selectivity versus SIK1.
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DC73148 JRD-SIK1/2i-4
JRD-SIK1/2i-4 is a potent, highly selective SIK1/2 inhibitor, modulates innate immune activation and suppress intestinal inflammation.
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DC73147 GLPG3312
GLPG3312 is a potent and selective pan-SIK inhibitor with IC50 of 2.0/0.7/0.6 nM for SIK1/SIK2/SIK3, respectively.
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DC73144 EB-42168
EB-42168 is a potent, selective G2019S-LRRK2 kinase inhibitor with IC50 of 1.1 nM (pS935-LRRK2) in FRET-based assay, >100-fold selective over WT-LRRR2.
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DC73142 DC-ATG4in
DC-ATG4in is a small molecule autophagy related 4B (ATG4B) inhibitor, directly binds to ATG4B and inhibits its enzyme activity with IC50 of 3.08 uM, DC-ATG4in is an autophagy inhibitor.
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DC73141 YTK-2205
YTK-2205 (YTK2205) is a small molecule p62 agonist targeting ZZ domain, induces selective autophagy activation, YTK-2205 augments the translocation of p62 to mitochondria, targeting their lysosomal degradation.
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DC73140 RH1115
RH1115 is a small molecule activator and inducer of autophagy targeting Lamin A/C and LAMP1, induces changes to LAMP1 vesicle properties and alters lysosome positioning.
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DC73139 JS-017
JS-017 (JS017) is a small molecule degrader of N-retinylidene-N-retinylethanolamine (A2E), one of the components of lipofuscin, degrades A2E-BDP from ARPE-19 cells with IC50 of 3.239 uM.
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DC73138 Zharp2-1
Zharp2-1 is a novel potent, selective RIPK2 inhibitor with IC50 of 38.5 nM in ADP-Glo kinase assay, effectively blocks RIPK2 kinase function and NOD-mediated NF-κB/MAPK activation.
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DC73137 Zharp1-211
Zharp1-211 is a potent, selective, type II inhibitor of RIPK1 kinase with IC50 of 53 nM and binding Kd of 8.7 nM.
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DC73136 Oditrasertib
Oditrasertib is a potent, selective RIPK1 inhibitor.
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DC73135 GSK2593074A
GSK2593074A (GSK'074, GSK-2593074A) is novel potent, selective RIP1/RIP3 kinase dual inhibitor, directly binds to RIP1 and RIP3 with Kd of 130 and 12 nM, respectively.
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DC73133 Flizasertib
Flizasertib is a potent, selective RIP1 kinase (RIPK1) inhibitor with potential for treating prophylaxis.
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DC73132 cRIPGBM chloride
cRIPGBM (RIPGBM derivative cRIPGBM, RIPGBM-18) is a metabolite of RIPGBM induces apoptosis in GBM CSCs (EC50=68 nM in GBM 1 cells) by interacting with RIPK2 (Kd=2.3 uM).
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DC73131 aYM155
aYM155 is a brain-penetrating prodrug form of YM155 (Cat. PC-42439, potent survivin inhibitor), displays potent cell killing activity against a broad panel of patient-derived GBM cancer stem-like cells (IC50=0.7-10 nM).
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DC73129 UCI-LC0023
UCI-LC0023 is a small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.
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DC73128 UCI-LC0019
UCI-LC0019 is a specific small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.
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DC73127 UC2288
UC2288 is a small molecule p21 inhibitor, attenuates p21 protein abundance at 10 µM, independently of p53 activity and at the level of transcription or post-transcription.
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DC73126 ReACp53
ReACp53 is a cell-penetrating 17-residue peptide designed to inhibit p53 amyloid formation, rescues p53 function in cancer cell lines.
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DC73125 NSC146109
NSC146109 (XI-011) is a small-molecule p53 activator, induces apoptosis of breast cancer cells through inhibiting MDMX (MDM4) expression.
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DC73124 Morncide
Morncide (Morn3 (222-237)) is a cell-penetrating, 16-AA Morn3-targeting peptide that disrupts the interaction between p53 and Morn3-mediated complex, Morncide peptide stabilizes and reactivates p53 in cancer cells.
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DC73123 MMRi71
MMRi71 is a small molecule inhibitor of the E3 ligase activity of MDM2-MDM4, and an inducer of MDM4 and FTH1 dual protein degradation and p53-independent apoptosis in leukemia cells.
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DC73122 MMRi67
MMRi67 is a potent E3 ligase inhibitor of the MDM2-MDM4 E3 complex, inhibits RING-RING interaction of MDM4 and MDM2B with Kd of 896 nM.
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DC73121 K-181
K-181 is a specific small-molecule Protein-Protein Interaction (PPI) inhibitor of Mdmx-p53 interaction, exhibits neuroprotective effects on ischemic stroke by disrupting Mdmx-p53 interaction and inhibiting HDAC6 activity.
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DC73119 GY1-22
GY1-22 is a small molecule inhibitor against DNAJA1-mutP53R175H interacting pocket, reduces mutp53 protein expression in colon cancer cell line with p53R175H mutation.
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DC73118 BAY 249716
BAY 249716 is a small molecule that modulate mutant p53 condensation, showed significant stabilization of all three p53 protein variants, p53WT p53R175H and p53Y220C.
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DC73116 RMT 5265
RMT 5265 (RMT5265) is a potent, small molecule bivalent mimic of Smac, inhibits XIAP and cIAP1/2 through the BIR3 domain.
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DC73114 ARTS mimetic A4
ARTS mimetic A4 is a small molecule that mimics the function of the pro-apoptotic ARTS (Sept4_i2) protein, binds the ARTS pocket in XIAP-BIR3, but not cIAP1, specifically promotes degradation of XIAP and induces caspase-mediated cell death.
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DC73113 142D6
142D6 is a potent, Lys-covalent pan-IAP inhibitor, targets the BIR3 domain of the inhibitor of the apoptosis protein (IAP) family with IC50 of 43/21/21 nM for XIAP/cIAP1/cIAP2, respectively.
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