| DC50249 |
Monoacylglycerol lipase inhibitor 1 |
Monoacylglycerol lipase inhibitor 1 is a potent monoacylglycerol lipase inhibitor (compound 13). |
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| DC50259 |
Geodin |
Geodin, a fungal metabolite, shows antibacterial activity. Geodin also is an inhibitor of plasminogen activator inhibitor- 1 (PAI-1). |
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| DC50262 |
Trichomide A |
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases. |
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| DC50263 |
Rubratoxin A |
Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts. |
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| DC50264 |
(S)-GDC-1971 |
SHP2 inhibitor is an effective SHP2 allosteric inhibitors (IC50≤50 nM), blocking the activation of SHP2 by targeting the auto-inhibited conformation of SHP2 (WO2019183367A1, compound 118). |
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| DC50265 |
GDC-1971
Featured
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GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.
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| DC50266 |
(S)-ABBV-CLS-484 |
(S)-ABBV-CLS-484 is a potent PTPN1 or PTPN2 inhibitor. |
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| DC50268 |
SHP2-IN-9 |
SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo. |
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| DC70079 |
GSK2973980A |
GSK2973980A is a potent and selective DGAT1 inhibitor with IC50 of 3 nM, exhibits >2,900-fold selectivity over human DGAT2, ACAT1 and ACAT2 (IC50>10 uM). |
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| DC70084 |
GSK 2793660 |
GSK 2793660(GSK2793660) is a potent, selective, irreversible and orally bioavailable cathepsin C inhibitor, but not the activity of downstream neutrophil serine proteases, for the treatment of cystic fibrosis, non-cystic fibrosis bronchiectasis, ANCA-associated vasculitis and bronchiectasis.. |
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| DC70086 |
GSK-484
Featured
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GSK-484 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 80 nM in FP binding assay (0.2 mM Ca), 50 nM in PAD4 NH3 release inhibition assay. |
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| DC70090 |
GLPG1972 |
GLPG1972 (Aldumastat, S201086) is a potent and selective small-molecule inhibitor of ADAMTS5 with IC50 of 19 and <23 nM against human and rat ADAMTS5, respectively. |
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| DC70093 |
WX-UK1 |
WX-UK1 (UKI-1) is a small synthetic serine protease uPA (urokinase-type plasminogen activator) inhibitor that blocks tumor cell invasion, metastasis and primary tumor growth. |
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| DC70105 |
NSC45586 free base |
NSC45586 free base (NCS 45586, NCI45586) is a potent, specific PHLPP2 inhibitor with IC50 of 4 uM, targets the PHLPP2 PP2C domain, suppresses MYC and triggers cell death. |
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| DC70119 |
8-BOA |
8-BOA is a selective and potent mechanism-based inactivator of breast cancer-associated CYP4Z1.8-BOA exhibited favourable inhibitory activity in vitro, thus meriting in vivo characterization. |
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| DC70121 |
Fumarase-IN-2 sodium |
A cell-permeable small molecule inhibitor of Fumarase (fumarate hydratase), an enzyme of the tricarboxylic acid cycle (TCA cycle); elicits a nutrient-dependent cytotoxicity in a number of cancer cell lines, and displays increased growth-inhibitory activity toward SW620 cell line grown in the absence of glucose (mean IC50=2.2 uM). |
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| DC70126 |
GSK 366 |
A novel potent kynurenine-3-monooxygenase (KMO) inhibitor with IC50 of 2.3 nM and 0.7 nM for human KMO and Pf-KMO, respectively. |
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| DC70127 |
GSK 065 |
A novel potent kynurenine-3-monooxygenase (KMO) inhibitor with IC50 of 4.5 nM. |
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| DC70144 |
GSK-256066 |
A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively; displays >380,000-fold selectivity over PDE1/23/5/6/7; inhibits TNFα production by lLPS-stimulated human peripheral blood monocytes with IC50 of 0.01 nM; inhibites LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats. |
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| DC70145 |
GSK-2181236A |
A potent, selective soluble guanylate cyclase (sGC) stimulator that increases sGC activity (cGMP formation) with EC50s of 27 and 25 nM for rat and human sGC, respectively; displays 23-fold selectivity for sGC over OATP1B1 and >197-fold selectivity over a panel of 38 proteins; increases P-VASP levels in rat aortic smooth muscle cells with EC50 of 12.7 nM; attenuates the development of cardiac hypertrophy in a blood pressure-independent fashion. |
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| DC70163 |
A-908292 |
A-908292 is a highly potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor with IC50 of 38 nM (hACC2), no activity against ACC1 (IC50>30 uM). |
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| DC70165 |
AA6216 |
AA6216 (AA 6216) is novel potent, selective PDE4 inhibitor with IC50 of 0.63 nM.AA6216 showed stronger inhibitory effects against PDE4 than other PDE family members. AA6216 potently inhibits cytokine production (TNF-α,IL-12p40, IL-4, and IL-13, IC50s=2.2-7.9 nM) by PBMCs stimulated with PHA.AA6216 inhibited the production of TGF-β1 by a human monocytic cell line THP-1, AA6216 dose-dependently reduced the production of TNF-α by alveolar macrophages from patients with IPF.AA6216 demonstrated anti-fibrotic potency on mouse model of bleomycin-induced lung fibrosis. |
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| DC70169 |
AC1-IN-38
Featured
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AC1-IN-38 is a potent, selective inhibitor of adenylyl cyclase type 1 (AC1) with IC50 of 0.54 uM.AC1-IN-38 shows selectivity over a closely related isoform AC8, and no activity against AC2/5 and other common neurological targets.AC1-IN-38 displayed modest antiallodynic effects in a mouse model of inflammatory pain. |
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| DC70172 |
ACC2 inhibitor 2e |
ACC2 inhibitor 2e is a highly potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor with IC50 of 1.9 nM and 1950 nM for ACC2 and ACC1, respectively.ACC2 inhibitor 2e exhibited good PK profile and in vivo antidiabetic efficacy in C57BL/6 mice. |
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| DC70174 |
ADAM17 inhibitor SN-4
Featured
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ADAM17 inhibitor SN-4 is a newly identified, highly specific inhibitor of ADAM17 (A disintegrin and metalloproteinase 17), demonstrating potent activity in blocking TNF-α cleavage in cellular assays with an IC50 value of 3.22 µM. This compound exhibits slightly greater efficacy compared to marimastat, a well-established ADAM17 inhibitor. In vitro studies reveal that SN-4 effectively suppresses ADAM17-mediated cleavage of tumor necrosis factor α (TNF-α) and CD44, while showing no significant impact on ADAM10 activity. Additionally, SN-4 has been shown to inhibit cellular invasion, highlighting its potential as a targeted therapeutic agent for modulating ADAM17-related pathways. |
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| DC70180 |
KS100 |
ALDH inhibitor KS100 (KS100) is a novel, potent, multi-isoform ALDH inhibitor with IC50 of 207/1410/240 nM for ALDH1A1/ALDH2/ALDH3A1, respectively;
KS100 was mitigated by development of a nanoliposomal formulation, called NanoKS100. NanoKS100 was 5-fold more selective for killing melanoma cells compared with normal human fibroblasts. Inhibition by KS100 significantly reduced total cellular ALDH activity to increase reactive oxygen species generation, lipid peroxidation, and accumulation of toxic aldehydes leading to apoptosis and autophagy. |
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| DC70188 |
AM6580 |
AM6580 is a potent, covalent monoacylglycerol lipase (MAGL) inhibitor with IC50 of 3 nM (hMAGL).AM6580 covalently binds to and inactivates MAGL by carbamylation of the enzyme's catalytic Ser122 nucleophile. |
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| DC70189 |
AM9928 |
AM9928 is a potent, covalent monoacylglycerol lipase (MAGL) inhibitor with IC50 of 8.9 nM (hMAGL).AM9928 covalently binds to and inactivates MAGL by carbamylation of the enzyme's catalytic Ser122 nucleophile.AM9928 inhibited adhesion and transmigration of breast cancer cells through human brain microvascular endothelial cells (HBMECs), inhibited TNBC's secretion of inflammatory cytokines such as IL-6 and IL-8, and the angiogenic factor VEGF-A.AM9928 inhibited in vivo changes in BBB permeability and decreased TNBC colonization in brain.MAGL inhibitor AM9928 is a novel treatment of TNBC tumor growth and TNBC-colonization in the brain. |
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| DC70220 |
Asundexian
Featured
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Asundexian, also known as BAY2433334 and BI1265162, is a blood coagulation factor XIa inhibitor. Asundexian binds directly to the active site of FXIa and thereby inhibits its activity. |
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| DC70226 |
AXKO-0046 |
AXKO-0046 (AXKO0046) is the first highly selective, small molecule inhibitor of human lactate dehydrogenase B (LDHB), exhibits uncompetitive LDHB inhibition with EC50 of 42 nM.AXKO-0046 selectively inhibited LDHB activity in an uncompetitive manner with respect to NADH and pyruvate, no inhibitory activity against LDHA at 300 uM.AXKO-0046 did not bind in the catalytic site of the enzyme but significantly bound to LDHB in the novel allosteric site of the tetramer.AXKO-0046 is a promising chemical probe to elucidate the role of LDHB-associated pathways in cancer metabolism. |
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