Active Biopharma Corp

Ketorolac(RS37619), a non-selective COX inhibitor, is a non-steroidal anti-inflammatory drug.

Naratriptan is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches. Target: 5-HT1 Receptor Naratriptan is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches.

Ketorolac (Ketorolac tromethamine, Toradol) is a non-selective COX inhibitor with strong analgesic activity. Target: COX Ketorolac or ketorolac tromethamine is a non-steroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives, used as an analgesic.

Stavudine is a nucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV. Target: HIV RT; NRTIs Stavudine is a dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.

Naratriptan hydrochloride is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches. Target: 5-HT1 Receptor Naratriptan is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches.

Delafloxacin (RX-3341, ABT-492) is a fluoroquinolone antibiotic agent. IC50 Value: MICs ranging from 0.0078 to 0.125 micro g/ml for levofloxacin-resistant Streptococcus pneumoniae strains [1] Target: Antibacterial ABT-492 was more potent against quinolone-susceptible and -resistant gram-positive organisms, had activity similar to th...

CP-547632 is as a potent inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases (IC50 11 and 9 nM, respectively).

CHIR-98014 is a selective GSK3 inhibitor with IC50s of 0.65 nM and 0.58 nM for GSK-3α and GSK-3β; potentiate insulin activation of glucose transport and utilization in vitro and in vivo. IC50 value: 0.65 nM/0.58 nM (GSK-3α/GSK-3β) [1] Target: GSK-3α/GSK-3β Exposure of insulin receptor–expressing CHO-IR cells or primary rat hepatocyt...

RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively. IC50 Value: 23 nM Target: ALK5 in vitro: Pretreated MEFs with RepSox, applying the chemical for three days, and then removed it at the time of transduction...

LDN193189(DM 3189) is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. IC50 value: 5 nM/30 nM (ALK2/ALK3) [1] Target: ALK2/3 in vitro: LDN193189 potently inhibits BMP4-med...

Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of <b>VEGFR2</b>, <b> VEGFR3</b>, <b>PDGFα</b>, and <b>c-Kit</b> with <b>IC₅₀</b>s of 6, 4, 15 and 1 nM, respectively.

BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B.

LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2. IC50 value: 38 nM/300 nM(Ki, TβRI/II) [1] Target: TGF-β receptor type I/II in vitro: LY2109761 treatment induces a dose-dependent low-anchorage growth in...

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM; >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2.

PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively.

Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM; has >200-fold higher selectivity for Aurora A than Aurora B. IC50 Value: 1.2 nM (Aurora A) Target: Aurora A in vitro: MLN8237 (0.5 μM) treatment inhibits the phosphorylation of Aurora A in MM1.S and OPM1 cells, without affecting the Aurora B mediated histone ...

Selumetinib (AZD6244; ARRY-142886) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. IC50 value: 14 nM [1] Target: MEK1 in vitro: ZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphoryl...

ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM. IC50 Value: ≤ 0.5 nM(Ki for Bcl-xL); ≤1 nM(Ki for Bcl-2); ≤1 nM(Ki for Bcl-w) Target: Bcl-2 Family in vitro: ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, r...