| DC73207 |
PSB-0952 |
PSB-0952 (PSB0952) is a potent, selective ecto-5'-Nucleotidase (eN, CD73) inhibitor with Ki of 260 nM, >150-fold selectivity over NTPDases and P2Y receptor subtypes P2Y2, P2Y4, P2Y6, and P2Y12. |
|
| DC73208 |
PSB-0963 |
PSB-0963 (PSB0963) is a potent, selective ecto-5'-Nucleotidase (eN, CD73) inhibitor with Ki of 150 nM, >100-fold selectivity over NTPDases. |
|
| DC73209 |
TH6342 |
TH6342 (TH-6342) is a specific small-molecule inhibitor against the dNTP triphosphohydrolase (dNTPase) SAMHD1, inhibits the enzymatic activities of SAMHD1 against dGTP, Cl-F-ara-ATP, and ara-CTP with IC50 of 9.6, 11.0 and 5.8 uM, respectively. |
|
| DC73210 |
TH7528 |
TH7528 (TH-7528) is a specific small-molecule inhibitor against the dNTP triphosphohydrolase (dNTPase) SAMHD1, inhibits the enzymatic activities of SAMHD1 against dGTP, Cl-F-ara-ATP, and ara-CTP with IC50 of 4.5, 2.8 and 2.6 uM, respectively. |
|
| DC73211 |
AMXI-5001 |
AMXI-5001 (AMXI 5001) is a novel, highly potent, orally active dual PARP1/2 (IC50 5/0.05 nM) and microtubule polymerization inhibitor, inhibits intracellular PAR formation with IC50 of 7 nM. |
|
| DC73212 |
G-631 |
G-631 is a potent and selective TNKS1/2 inhibitor with IC50 of 7 nM in biochemical assays of tankyrase auto-PARsylation activity, and cellular potency of 8 nM (HEK293). |
|
| DC73213 |
KMR-206 |
KMR-206 (KMR206) is a potent, selective PARP7 inhibitor with IC50 of 13.7 nM, displays 75-fold selectivity for PARP7 over PARP2 and does not inhibit PARP1 up to 3 uM. |
|
| DC73214 |
kt-3283 |
kt-3283 is a novel bi-functional PARP-HDAC inhibitor with IC50 of 0.338 nM, 2.19 nM and 1.89 uM for PARP1, PARP2 and HDACs, respectively. |
|
| DC73215 |
Mortaparib |
Mortaparib is a dual inhibitor of mortalin-PARP1 interaction, and a p53 activating cytotoxic compound, induces activation of growth arrest and apoptosis signaling in cancer cells in vitro and in vivo. |
|
| DC73216 |
Mortaparib Plus |
Morataprib Plus is a novel anticancer small molecule that disrupts mortalin-p53 interaction, prevents the interaction of mortalin with p53 resulting in the activation of growth arrest and apoptosis mediated by activation of p21WAF1 or BAX and PUMA signall |
|
| DC73218 |
HC-5404 |
HC-5404 (LY-4) is a potent, selective and orally active inhibitor of PKR-like endoplasmic reticulum kinase (PERK, EIF2AK3) with IC50 of 1 nM. |
|
| DC73219 |
Allopole
Featured
|
Allopole is the first allosteric, specfic and cell-permeable inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1), Allopole is the prodrug of Allopole-A. |
|
| DC73220 |
Allopole-A |
Allopole-A is the first allosteric, specfic inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1) with IC50 of 2.5 nM in FP-based assays, Allopole-A is the active form of Allopole. |
|
| DC73221 |
SBE13 |
PLK1 inhibitor SBE13 is a potent, selective PLK1 inhibitor with IC50 of 0.2 nM, with little to no inhibition against PLK2/PLK3 (IC50, 65 uM/875 nM). |
|
| DC73222 |
(R)-BA-1049 |
(R)-BA-1049 is a potent, orally-available ROCK2-selective inhibitor with IC50 of 0.24 uM, 16-fold selectivity over ROCK-1. |
|
| DC73223 |
(S)-BA-1049 |
(S)-BA-1049 is a potent, orally-available ROCK2-selective inhibitor with IC50 of 0.24 uM, 16-fold selectivity over ROCK-1. |
|
| DC73224 |
C3TD879 |
C3TD879 is a potent, selective first-in-class Citron kinase (CITK) chemical inhibitor with biochemical IC50 of 12 nM. |
|
| DC73225 |
ITRI-E-(S)4046 |
ITRI-E-(S)4046 (E(S)4046) is a potent, highly specific, dual synergistic inhibitor of myosin light chain kinase 4 (MYLK4) and Rho-related protein kinase (ROCK) with IC50 of 3.2 nM and 25.6 nM for ROCK1 and MYLK4, respectively. |
|
| DC73226 |
Netarsudil |
Netarsudil (AR-13324) is a potent, selective ROCK inhibitor with Ki of 4.2 nM for ROCK2. |
|
| DC73227 |
DIZ-3 |
DIZ-3 is a dimeric aryl-substituted imidazole as a selective multimeric G-quadruplex (G4) ligand, intercalates into the G4-G4 interface, induces cell cycle arrest and apoptosis, and inhibits cell proliferation in alternative lengthening of telomere (ALT) |
|
| DC73228 |
Teloxantron |
Teloxantron (Telomerase inhibitor TXT4) is a potent small molecule inhibitor of telomerase activity with IC50 of 9.61 uM, 7-fold lower than BIBR1532 (Cat# PC-45170), inhibits the processivity of telomerase with preferential DNA damage on telomeres. |
|
| DC73229 |
LMP744 |
LMP744 (MJ-III-65, NSC706744) is a small molecule TOP1 inhibitor antitumoral activity. |
|
| DC73230 |
SD133 |
SD133 (Sd-133) is a drug-like small molecule inhibitor of adhesion molecule cadherin 11 (CDH11), binds specifically to the CDH11 binding pocket with KD of 25.2 uM in SPR assays. |
|
| DC73231 |
GB1490 |
GB1490 is a potent, selective and orally available galectin-1 (gal-1) inhibitor with Kd value of 0.4 uM and 0.23 uM for human and mouse galectin-1, respectively. |
|
| DC73232 |
6-B345TTQ |
6-B345TTQ is a small molecule inhibitor of the α4 integrin-paxillin interaction, impairs the interaction of native paxillin with α4 integrin, decreases α4-mediated cell migration. |
|
| DC73233 |
7HP349 |
Alintegimod (7HP349) is a small molecule activator of the integrins αLβ2 (LFA-1) and α4β1 (VLA-4). 7HP349 directly activates integrin cell adhesion receptors crucial for the generation of an immune response. |
|
| DC73234 |
A7B7C7 |
A7B7C7 (11-A7B7C7) is a potent Paxillin-α4 integrin binding antagonist with IC50 of 300 nM in vitro, decreases α4β1-mediated T cell migration. |
|
| DC73235 |
AXT107 |
AXT107 (AXT-107) mimetic peptide derived from collagen IV, binds integrins αvβ3 and α5β1 (Kd=1.29 and 2.21 nM), disrupts VEGFR2-β3 complex formation. |
|
| DC73236 |
GSK3335103
Featured
|
GSK3335103 is a highly potent and orally bioavailable nonpeptidic αvβ6 integrin inhibitor with pIC50 of 8.0. GSK3335103 shows high desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance, moderate volumes of distributio, high to complete oral bioavailabilities and high solubility in all physiological media. |
|
| DC73237 |
GW559090 |
GW559090 is a potent, selective, competitive and high-affinity α4β1 integrin (VLA-4) antagonist with Kd of 0.19/1.04 nM for huamn/rat α4β1, respectively. |
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