STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.IC50 value:Target: NAMPT inhibitorin vitro: improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia, and targets leukemia stem cells. STF-118804 displays distinctive cytotoxicity by inducing apoptosis without causing a phase-specific cell cycle arrest. Over-expression of NAMPT rendered 293T cells more resistant to STF-118804 resulting in a higher IC50 (106 nM, 95% CI 74–151 nM) compared to control cells (17 nM, 95% CI 13–23 nM), further confirming that NAMPT protein levels dictate sensitivity to STF-118804 [1].in vivo: STF-118804 displayed high efficacy in a xenograft model of ALL. Mice treated with STF-118804 over a 20-day period survived an average of 34 days longer than vehicle-treated animals. During treatment, bioimaging showed regression of tumor followed by suppression of disease. STF-118804 was tolerated in the efficacious dose range, and the absence of adverse physical or pathological effects indicated that toxicity was not limiting in a 20-day study of mock transplanted mice [1].
IDO1/TDO-IN-2 (Compound 1) is a potent inhibitor of IDO1/TDO with IC50s of 0.1 and 0.07 μM. IDO1/TDO-IN-2 has the potential for the research of cancer diseases[1].
Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
Benzophenonetetracarboxylic acid can inprove activity and stability of alkaline phosphatases from psychrophilic and mesophilic organisms.Benzophenonetetracarboxylic acid can improve activity and stability of alkaline phosphatases from psychrophilic and mesophilic organisms by chemically modifying aliphatic or amino groups
Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir. Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.36 μM[1][2].
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research[1][2].
KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells[1].
D-Tyrosine-d2 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting[1].
7-Ethoxy-4-methylcoumarin is a coumarin derivative and can be used as a substrate probe of mammalian cytochromes P450 1A1, 2B4 and 2B6[1][2].
From the myxobacterium Lysobacter enzymogenes. In peptidase family S1 (trypsin family) Reaction: Preferential cleavage: Ala┼, Val┼ in bacterial cell walls, elastin and other proteins
Tigulixostat is a novel (indolyl)heteroarylcarboxylate derivatives effective as non-purine selective xanthine oxidase inhibitor, which lowers the production of uric acid[1].
5-Hydroxyferulic acid is a hydroxycinnamic acid and is a metabolite of the phenylpropanoid pathway. 5-Hydroxyferulic acid is a precursor in the biosynthesis of sinapic acid and is also a COMT non-esterifed substrate[1][2][3].
Galangin is an agonist/antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.
AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.)Target: RARα agonistCompound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation.Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, compound 4 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients.
(Rac)-5-Keto Fluvastatin (3-Hydroxy-5-Keto Fluvastatin) is an impurity of Fluvastatin (XU 62320). Fluvastatin is a HMG-CoA reductase inhibitor with an IC50 of 8 nM[1].
Sacubitrilat is an active neprilysin (NEP) inhibitor.
(-)-Hydroxycitric acid (Garcinia acid) is the principal acid of fruit rinds of Garcinia cambogia. (-)-Hydroxycitric acid is a potent and competitive inhibitor of ATP citrate lyase. (-)-Hydroxycitric acid suppresses the fatty acid synthesis, lipogenesis, food intake, and induced weight loss[1][2].
hCAXII-IN-2 (compound 5i) is a potent human carbonic anhydrase XII (hCA XII) and hCA IX inhibitor with Ki values of 84.2 nM and 268.5 nM, respectively. hCAXII-IN-2 shows less active against hCA I and hCA II[1].
SR1078 is an agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ).
PF-05085727 is a potent, selective and brain penetrant Phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 2 nM.
(S)-SBFI-26 is the (S) enantiomer of SBFI-26, an anti-nociceptive agent binds to anandamide transporters FABP5 and FABP7. (S)-SBFI-26 has anti-nociceptive and anti-inflammatory effects[1].
Ursodeoxycholic acid-13C is the 13C labeled Ursodeoxycholic acid. Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active[1][2].
U-73122 is an inhibitor of phospholipase C (PLC), phospholipase A2, and 5-LO (5-lipoxygenase).
HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1[1].
Diprotin A (TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 μM.
PF-3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 μM); showing negligible activity against FAAH2.IC50 value: 0.23 uMTarget: FAAHPF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile [1]. PF-3845 treated mice (10 mg/kg, i.p.) shows rapid and complete inactivation of FAAH in the brain, as judged by competitive activity-based protein profiling (ABPP) with the serine hydrolase-directed probe fluorophosphonate (FP)-rhodamine. PF-3845 shows a long duration of action up to 24 hour. PF-3845-treated mice also shows dramatic (>10-fold) elevation in brain levels of AEA and other NAEs (N-pamitoyl ethanolamine [PEA] and N-oleoyl ethanolamine [OEA]). FAAH is AEA-degrading enzyme fatty acid amide hydrolase. PF-3845 (1–30 mg/kg, oral administration [p.o.]) causes a dose dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg (rats are analyzed at 4 hour post dosing with PF-3845). At higher doses (10 and 30 mg/kg), PF-3845 inhibits pain responses to an equivalent, if not greater, degree than the nonsteroidal anti-inflammatory drug naproxen (10mg/kg, p.o.) [1]. PF-3845 (10 mg/kg, i.p.) significantly reverses LPS-induced tactile allodynia, but doesn't modify paw withdrawal thresholds in the saline-injected paw [2].
Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
Aeruginosin 98-B is a protease inhibitor. Aeruginosin 98-B inhibits trypsin, plasmin and thrombin with IC50 values of 0.6, 7.0 and 10.0 μg/mL, respectively[1].