Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc[1].
Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against MCF-7 human breast cancer cells, breast cancer cell line (MDA-MB-231), but not normal human skin fibroblasts[1][2][3].
VO-OHPic is a reversible, noncompetitive and selective PTEN inhibitor with an IC50 of 46 nM. VO-OHPic attenuates apoptosis, adverse cardiac remodeling, and pro-inflammatory M1 macrophages in doxorubicin-induced cardiomyopathy. VO-OHPic inhibits autophagy[1][2][3].
PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer[1].
UCD38B hydrochloride is a cell permeant, competitive enzymatic uPA inhibitor with an IC50 value of 7 μM. UCD38B hydrochloride targets intracellular uPA causing mistrafficking of uPA into perinuclear mitochondria, reducing the mitochondrial membrane potential, and followed by the release of apoptotic inducible factor (AIF). UCD38B hydrochloride induces apoptosis[1][2].
RGT-068A is a potent, selective and oral bioavailable MALT1 inhibitor[1].
Bavachalcone is a major bioactive compounds isolated from Psoralea corylifolia L.; has been widely used as traditional Chinese medicine; antibiotic or anticancer agent.IC50 value:Target:Bavachalcone inhibited osteoclast formation from precursor cells with the IC(50) of approximately 1.5 microg ml(-1). The activation of MEK, ERK, and Akt by receptor activator of nuclear factor kappaB ligand (RANKL), the osteoclast differentiation factor, was prominently reduced in the presence of bavachalcone. The induction of c-Fos and NFATc1, key transcription factors for osteoclastogenesis, by RANKL was also suppressed by bavachalcone [1]. Bavachalcone exhibited a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro [2]. Bavachalcone had stronger inhibition on UGT1A1 and UGT1A7 than corylin which did not inhibit UGT1A1, UGT1A3, UGT1A7, UGT1A8, UGT1A10, and UGT2B4. Data fitting using Dixon and Lineweaver-Burk plots demonstrated the noncompetitive inhibition of bavachalcone against UGT1A1 and UGT1A7-mediated 4-MU glucuronidation reaction. The values of inhibition kinetic parameters (Ki) were 5.41 μ M and 4.51μ M for UGT1A1 and UGT1A7, respectively [3].
SKLB4771 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.IC50 value: 10 nM (in vitro) [1]Target: in vitro: SKLB4771 inhibited FLT3 phosphorylation in a dose-dependent manner. Consistent with the downregulation of the phosphorylation of FLT3, the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 was also significantly inhibited at concentrations >0.1 μM. SKLB4771 potently inhibited the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. It just exhibited very weak inhibitory activity against human T lymphoma Jurkat cells, human Burkitt's lymphoma Ramos cells, human lung cancer PC-9 and H292 cells, and human epithelial carcinoma A431 cells (IC50: 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM, and 8.91 μM, respectively). For other leukemia and solid tumor cell lines, including K562, U937, Karpas299, HCC827, A549, H2228, H820, MDA-MB-231, BT474, MCF-7, HCT116, SW480, LoVo, HeLa, SKOV-3, SK, DU145, PC-3, A431, and SH-SY5Y [1].in vivo: Treatment with SKLB4771 at 100 mg/kg/d resulted in rapid and complete tumor regression in all mice of this group. SKLB4771 treatment at 20 mg/kg/d and 40 mg/kg/d significantly slowed down the tumor growth; the tumor inhibition rates are 66% and 84%, respectively. Moreover, during the whole experiment, no significant weight loss or any other obvious signs of toxicity were observed for all of the SKLB4771 treated mice.
8,8a-Dihydro-8-hydroxygambogic acid is a natural product, that can be isolated from the resin of Garcinia hanburyi. 8,8a-Dihydro-8-hydroxygambogic acid shows anticancer activity[1].
Enpp-1-IN-17 (example 274) is a potent ENPP1 inhibitor, with the inhibition constants (Ki values) toward cGAMP and ATP hydrolysis of 100 nM-1 μM and > 1 μM, respectively. The selectivity ratio for inhibition of cGAMP hydrolysis versus ATP hydrolysis is >6.4[1].
Quinate is an antiarrhythmic agent. Quinate is a potent, orally active, selective cytochrome P450db inhibitor. Quinate is also a K+ channel blocker with an IC50 of 19.9 μM. Quinate can be used for malaria research[1][2][3].
Ziyuglycoside II is a triterpenoid saponin compound extracted from Sanguisorba officinalis L.. Ziyuglycoside II induces reactive oxygen species (ROS) production and apoptosis. Anti-inflammation and anti-cancer effect[1].
AZD-1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of < 0.4 nM, selectively against JAK3 and Tyk2, and to a smaller extent against JAK1.
F16 is a small molecule that selectively inhibits proliferation of mammary epithelial, neu-overexpressing cells, as well as a variety of mouse mammary tumor and human breast cancer cell lines. 1, F16 induced cell cycle arrest in sensitive mouse tumor and human cancer cell lines.2, Prolonged incubation with 3 uM F16 resulted in increased cell death of F16-sensitive cells but not of F16-resistant ones.3, F16 caused apoptosis in A6 cells.4, F16 caused a dramatic decrease in the number of cells in S phase and an increase in the percentage of cells in G1 phase.5, F16 is capable of inhibiting oxidative phosphorylation and inducing mitochondrial transmembrane depolarization.
4,4'-Dimethoxybenzil is a human intestinal carboxyl esterase (hiCE) inhibitor with Ki of 70 nM.
Thymidine-13C-1 is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]
p53 Activator 3 (compound 87A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 3 can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA. p53 Activator 3 shows anti-tumor activity[1].
RPR132595A-d3 is the deuterium labeled RPR132595A. RPR132595A is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine[1][2].
AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth[1].
NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) is a topoisomerase I inhibitor, which can be delivered to cells through conjugated antibody targeting, and has good ADC activity in vivo and in vitro[1].
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.IC50 value: 5 nM [2]Target: WNTin vitro: CCT251545 is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases. CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM. CCT251545 is a small-molecule inhibitor of the WNT pathway discovered through cell-based screening. CCT251545 displays potent cell-based activity. CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1. [1] CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0 ± 0 μM). CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand or other stimulants (IC50 = 0.023 ± 0.011 μM and 0.190 ± 0.030 μM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 μM).[2]in vivo: CCT251545 as a potent and selective chemical probe suitable for cell-based exploration of the reported context-dependent roles of CDK8 and CDK19 and associated kinase module subunits in human disease and other biological settings. [1]
Enapotamab is an anti-AXL/UFO reference antibody. Enapotamab can be used to synthesis Bcl-xl inhibitor antibody-drug conjugates[1].
KAAD-Cyclopamine, a hedgehog signaling inhibitor, is a smoothened antagonist[1].
MRT68921 hydrochloride is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 µM and 56.26 µM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway[1].
Ginisortamab (UCB6114) is a fully human IgG4P antiGremlin-1 monoclonal antibody. Ginisortamab has the potential for the research of gastrointestinal (GI) tumors[1].
GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models[1].
Fz7-21S is a negative control of Fz7-21. Fz7-21 is a potent peptide antagonist of FZD7 receptors[1].
Ketotrexate sodium is an orally active antifolate and immunosuppressant. Ketotrexate sodium has good anti-inflammatory activity and is widely used in rheumatoid arthritis (RA). Ketotrexate sodium is used in research into cancer and autoimmune diseases[1][2].