Activators & Inhibitors

Activity: p38α MAP kinase inhibitor . Function/Pharmacology: A potent and selective inhibitor of p38 MAP kinases, p38 MAPK and p38 (KD = 3.7 and 17 nM respectively).1 Inhibits IL-6, IL-1 and TNF production in LPS-primed blood.1 Inhibits p38 in platelets stimulated by thrombin, collagen or thromboxane agonist U-46619 at 1 M.2 Provides only modest clinical efficacy in rheumatoid arthritis.3,4 Delays platelet lesions and leads to better maintenance of stored platelets.5 Chemical Name: 6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide

Activity: Sonic Hedgehog signaling pathway inhibitor . Function/Pharmacology: A potent and selective Hedgehog (Hh) pathway signaling inhibitor antagonizing SMO with a Ki of 1.3 nM).1 Alters intracellular Ca2+ homeostasis and inhibits growth of cisplatin-resistant lung cancer cells.2 Inhibits two ABC transporters, ABCG2/BCRP and ABCB1/Pgp, IC50s=1.4 and 3.0 μM respectively.3 Clinically useful for the treatment of basal cell carcinoma.4 Inhibits proliferation and induces apoptosis in colon cancer cell lines. Chemical Name: 2-Chloro-N-(4-chloro-3-(pyridine-2-yl)phenyl)-4-(methylsulfonyl)benzamide

Activity: VEGFRK inhibitor . Function/Pharmacology: Potent, selective inhibitor of the VEGFR tyrosine kinases VEGFR-1 (Flt-1, IC50 = 77 nM) and VEGFR-2 (FLK-1/KDR, IC50 = 37 nM)1. Weaker inhibitor of other tyrosine kinases including PDGFR-β (IC50 = 580 nM), c-KIT (IC50 = 730 nM), FLT-4 (IC50 = 660 nM) and c-FMS (IC50 = 1.4 µM). Inactive against the EGFR, c-SRC, v-ABL, and protein kinase Cα (IC50 > 10 µM). Inhibits the growth of multiple myeloma cells in the bone marrow microenvironment2. Chemical Name: N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine dihydrochloride

Activity: VEGFRK inhibitor . Function/Pharmacology: A potent and selective inhibitor of VEGFR2, (KDR IC50 = 40 nM). Also inhibits fms-like tyrosine kinase 4 (VEGFR3, IC50 = 110 nM) and epidermal growth factor receptor (EGFR/HER1, IC50 = 500 nM) but shows selectivity against a panel of other tyrosine and serine-threonine kinases. Inhibits colony formation in seven cancer cell lines2. Displays anti-angiogenesis activity3. Chemical Name: 4-(4-Bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-yl)methoxy]quinazoline

Activity: AP-1 transcription factor inhibitor . Function/Pharmacology: Diterpenoid naphthoquinone found in Salvia sp. and isolated as an active component of the traditional Chinese medicine Tanshen. Tanshinone IIA displays anti-inflammatory activity1 and induces apoptosis in a variety of cell lines2. Also inhibits AP-1 activity by suppressing jun-fos-DNA complex formation (IC50 = 0.22 µM)3. Chemical Name: 1,6,6-Trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]furan-10.11-dione

Activity: Proteasome inhibitor . Function/Pharmacology: Displays potent antioxidant and anti-inflammatory activity. Inhibits NFκB (IC50=270 nM). It induces heat shock response and cytoprotection in various cells. Inhibits 20S proteasome chymotrypsin activity (IC50=2.5 μM). Induces autophagy by targeting AR/miR-101 in prostate cancer cells.4 Induces UPR-dependent cell death in cancer cells.5 Cell permeable. Chemical Name: (9ß,13α,14ß,20α)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid

Activity: Survivin inhibitor . Function/Pharmacology: Induces apoptosis in a variety of cell lines acting as an antagonist of Bcl-2 family proteins (IC50 < 1 μM)1, however additional targets may contribute to its cytotoxicity. It suppresses cancer invasion and migration by inhibiting TGFβ1-induced epithelial-to-mesenchymal transition.2 Potentiates the chemosensitivity of cancer cells to other agents.3 Down-regulates surviving, reversing docetaxel resistance in cancer cells.4 Chemical Name: null

Activity: IGF1R inhibitor . Function/Pharmacology: Potent and selective inhibitor of insulin-like growth factor 1 receptor (IGF1R) which is non-competitive with ATP1. Displays no activity at IR, EGFR, FGFR or PDGFR. Inhibits IGF1R autophosphorylation IC50 ~ 1 nM1. Displays antiproliferative activity in numerous tumor cell lines, IC50 = 0.05 - 15 M2. Exhibits antiangiogenic activitiy3. Attenuates intimal hyperplasia after vascular injury4. Active in vivo. Chemical Name: (5R,5aS,8aR,9R)-5,8,8a,9-Tetrahydro¬-9-hydroxy-5-(3,4,5-trimethoxyphenyl)-furo[3',4':6,7¬]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one

Activity: Serine protease inhibitor, antiviral, anti-inflammatory activity . Function/Pharmacology: A serine protease inhibitor inhibiting plasmin, kallikrein, thrombin as well as trypsin, which attenuates pancreatic fibrosis.1 Reduces weight gain and improves metabolism in obese rodent models.2 In clinical use (in Japan) for pancreatitis.3 Inhibits influenza virus replication in human tracheal epithelial cells.4 Reduces infection of Calu-3 lung cells by SARS-CoV-2 (responsible for COVID-19) via inhibition of the serine protease TMPRSS2 required for viral spike protein priming.5 Chemical Name: 4-(2-(2-(Dimethylamino)-2-oxoethoxy)-2-oxoethyl)phenyl 4-guanidinobenzoate