S1579 |
Palbociclib (PD0332991) Isethionate |
Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. |
S2163 |
PF-4708671 |
PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported. |
S1216 |
PFI-1 (PF-6405761) |
PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay. |
S2128 |
Bazedoxifene (WAY-140424) HCl |
Bazedoxifene HCl (WAY-140424, TSE-424) is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively. |
S2224 |
UK 383367 |
UK-383367 is a procollagen C-proteinase inhibitor with IC50 of 44 nM, has excellent selectivity over MMPs. |
S2222 |
PF-3716556 |
PF 3716556 is a potent and selective P-CAB (potassium-competitive acid blocker), with pIC50 of 6.026 and 7.095 for the inhibition of porcine H+,K+-ATPase activity in ion-leaky and ion-tight assay, respectively, inhibits gastric acid secretion, displays no activity at Na+,K+-ATPase, used for the treatment of gastroesophageal reflux disease. |
S2921 |
PF-4981517 |
PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7. |
S2830 |
Clindamycin |
Clindamycin inhibits protein synthesis by acting on the 50S ribosomal, used for the treatment of bacterial infections. |
S1036 |
Mirdametinib (PD0325901) |
Mirdametinib (PD0325901) is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2. |
S1039 |
Rapamycin (AY-22989) |
Rapamycin (AY-22989, Rapamune, Sirolimus, NSC-2260804) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells. |
S1068 |
Crizotinib (PF-02341066) |
Crizotinib (PF-02341066) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. |
S1116 |
Palbociclib (PD-0332991) HCl |
Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. |
S1042 |
Sunitinib (SU11248) malate |
Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis. |
S1208 |
Doxorubicin (Adriamycin) HCl |
Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation. |
S5001 |
Tofacitinib (CP-690550) Citrate |
Tofacitinib citrate (CP-690550, Tasocitinib) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. Tofacitinib citrate has anti-infection activity. |
S1005 |
Axitinib (AG 013736) |
Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively. |
S1044 |
Temsirolimus (CCI-779) |
Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis. |
S1014 |
Bosutinib (SKI-606) |
Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy. |
S1264 |
PD173074 |
PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells. |
S1261 |
Celecoxib (SC 58635) |
Celecoxib (SC 58635) is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells. |
S2789 |
Tofacitinib (CP-690550) |
Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis. |
S2743 |
PF-04691502 |
PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2. |
S1196 |
Exemestane (FCE 24304) |
Exemestane (FCE24304, PNU155971) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively. |
S1408 |
Linezolid (PNU-100766) |
Linezolid (PNU-100766) is a synthetic antibiotic used for the treatment of serious infections. |
S2077 |
Atorvastatin Calcium |
Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin Calcium induces apoptosis and autophagy. |
S1403 |
Tigecycline (GAR-936) |
Tigecycline (GAR-936) is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline induces autophagy by downregulating the PI3K-AKT-mTOR pathway. |
S1331 |
Fluconazole (UK 49858) |
Fluconazole (UK 49858) is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections. |
S2777 |
PF-5274857 |
PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier. |
S2550 |
Tolterodine tartrate |
Tolterodine tartrate (PNU-200583E) is a tartrate salt of tolterodine that is a competitive muscarinic receptor antagonist. |
S2666 |
PF-3845 |
PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2. |
S1444 |
Ziprasidone HCl |
Ziprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder. |
S1338 |
Gabapentin HCl |
Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain. |
S1440 |
Varenicline Tartrate (CP 526555-18) |
Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction. |
S1508 |
Alprostadil |
Alprostadil (Prostaglandin-E1, PGE1, Edex, Muse, Liprostin) is used as a drug in the treatment of erectile dysfunction and has vasodilatory properties. It is a Prostaglandin Analog and Prostaglandin E1 Agonist. |
S1727 |
Levonorgestrel |
Levonorgestrel (D-Norgestrel) is a female hormone that prevents ovulation. |
S1733 |
Methylprednisolone (NSC-19987) |
Methylprednisolone (NSC-19987) is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis. |
S2717 |
CP-91149 |
CP-91149 is a selective glycogen phosphorylase (GP) inhibitor with IC50 of 0.13 μM in the presence of glucose, 5- to 10-fold less potent in the absence of glucose. |
S2133 |
Gabapentin |
Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain. |
S2457 |
Clindamycin HCl |
Clindamycin HCl inhibits protein synthesis by acting on the 50S ribosomal, used for the treatment of bacterial infections. |
S2792 |
Torcetrapib |
Torcetrapib (CP-529414) is a CETP inhibitor with IC50 of 37 nM, elevates HDL-C and reduces nonHDL-C in plasma. Phase 3. |
S1835 |
Azithromycin (CP-62993) |
Azithromycin (CP-62993, XZ-450) is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections. |
S1424 |
Prazosin HCl |
Prazosin HCl (cp-12299-1) is a competitive alpha-1 adrenoceptor antagonist, used to treat high blood pressure or benign prostatic hyperplasia. |
S1716 |
Glyburide (Glibenclamide) |
Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes. |
S1576 |
Sulfasalazine (NSC 667219) |
Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy. |
S1808 |
Nifedipine (BAY-a-1040) |
Nifedipine (BAY-a-1040) is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina. |
S2551 |
Sulbactam sodium |
Sulbactam sodium (Unasyn, CP-45899-2) is an irreversible β-lactamase inhibitor. |
S2048 |
Clindamycin Phosphate |
Clindamycin Phosphate (NSC 618653) is a lincosamide antibiotic for Plasmodium falciparum with IC50 of 12 nM. |
S4147 |
Azithromycin Dihydrate |
Azithromycin Dihydrate is an acid stable orally administered macrolide antimicrobial drug, structurally related to erythromycin. |
S2167 |
Bazedoxifene (TSE-424) acetate |
Bazedoxifene Acetate (WAY-140424, TSE-424) is a third generation selective estrogen receptor modulator (SERM). |
S2596 |
Clindamycin palmitate HCl |
Clindamycin palmitate HCl is a water soluble hydrochloride salt of the ester of clindamycin and palmitic acid and a lincosamide antibiotic. |
S2589 |
Miglitol |
Miglitol (BAY-M-1099) is an oral anti-diabetic drug. |
S1958 |
Sulbactam |
Sulbactam is a beta-lactamase inhibitor with an average IC50 of 0.8 μM. |
S2118 |
Ibutilide Fumarate |
Ibutilide Fumarate (U-70226E) is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm by induction of slow inward sodium current, which prolongs action potential and refractory period of myocardial cells. |