NBD-14270, a pyridine analogue, is a potent HIV-1 entry antagonist with an IC50 of 180 nM against 50 HIV-1 Env-pseudotyped viruses. NBD-14270 binds to HIV-1 gp120 and shows potent antiviral activity. NBD-14270 shows low cytotoxicity (CC50>100 μM)[1][2].
Mafenide hydrochloride is a sulfonamide-type medication used as an antibiotic.Target: AntibacterialMafenide is a sulfonamide-type medication. Mafenide works by reducing the bacterial population present in the avascular tissues of burns and permits spontaneous healing of deep partial-thickness burns. It is used to treat severe burns. It is used topically as an adjunctive therapy for second- and third-degree burns. It is bacteriostatic against many gram-positive and gram-negative organisms, including Pseudomonas aeruginosa. Some sources state that mafenide is more appropriate for non-facial burns, while chloramphenicol/prednisolone or bacitracin are more appropriate for facial burns [1-3].
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1(IC50= 5 nM) in cells.IC50 value: 5 nM [1]Target: MTH1 inhibitorTH588 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family or a panel of 87 enzymes, GPCRs, kinases, ion channels and transporter. TH588 has been shown to selectively kill a variety of cancer cell lines and with in vivo activity shown for TH588 in SW480 colorectal and MCF7 breast tumour xenografts.
7-Hydroxy-1-naphthalenesulfonate (potassium) is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
QUIN 2, Tetrapotassium Salt is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects[1][2].
Clomipramine (Chlorimipramine) is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD)[1].
AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.
Macozinone is a new drug candicate that inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043target: DprE1In vitro: PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. [1]In vivo: PBTZ169 can be suspend in 0.25% hydroxy-propylmethyl-cellulose. The administertration for PBTZ169 is 100 mg/kg by gavage. The MIC50 and MIC90 values were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL.[2] PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB). [3]
α/β-Hydrolase-IN-1 exhibits the best-in-class MICs of 50 μM (25 μg/mL) and 16 μM (8.4 μg/mL) against M. smegmatis and M. tuberculosis H37Ra, respectively.
Neuromuscular Disorder-Targeting Compound 1 is used in the research of neuromuscular disorders such as symptoms of fibromyalgia syndrome and chronic fatigue syndrome.
Drynachromoside A is a chromone glycoside. Drynachromoside A has biochemical effects on the osteoblastic (MC3T3-E1 cells) proliferation activities[1].
Isodaphnoretin B can be isolated from the roots of S. chamaejasme[1].
Azadirachtin, one of the most promising botanical insecticides, is widely used for pest control. Azadirachtin induces apoptosis in insect cell lines, including Sf9, SL-1 and BTI-Tn-5B1-4[1].
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity[1].
SB-203186 hydrochloride is a potent and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively[1][2][3].
SAH is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine.
Diisopropylammonium dichloroacetate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
CFT7455 is a highly potent and selective degarder of IKZF1/3 with cereblon binding IC50 of 0.4 nM and picomolar DC50.Treatment of the KiJK cell line of anaplastic large cell lymphoma (ALCL) with CFT7455 for 6 hours led to an 89% reduction in IKZF1 protein levels.CFT7455 demonstrated potent antiproliferative activity across a panel of NHL cell lines with MYC, BCL2, and/or BCL6 translocations or rearrangements.CFT7455 is an orally bioavailable.CFT7455 achieved improved in vivo potency and efficacy, including deeper and more durable tumor regressions in models of ALCL, diffuse large B-cell lymphoma (DLBCL) and MCL in xenograft models.
Metformin (hydrochloride) is an FDA approved first-line drug for the treatment of type 2 diabetes. Metformin decreases hepatic glucose production, mostly through a mild and transient inhibition of the mitochondrial respiratory-chain complex 1.
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity[1]. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice[2].
Ethyl 2-(2-chloroacetamido)acetate is a Glycine (HY-Y0966) derivative[1].
Daclatasvir is a potent HCV NS5A protein inhibitor, with mean EC50 values of 50 and 9 pM against genotype 1a and 1b replicons, respectively.
Kisspeptin-10, rat is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10, rat is a ligand for the rodent kisspeptin receptor (KISS1, GPR54). Kisspeptin-10 reduces Methotrexate-induced reproductive toxicity as a potential antioxidant compound[1].
Indomethacin-D4 (Indometacin-D4) is a deuterium labeled Indomethacin. Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1].
Metoprolol EP impurity O-d7 hydrochloride is the deuterium labeled 3,3'-(Isopropylazanediyl)bis(1-(4-(2-methoxyethyl)phenoxy)propan-2-ol)[1].
CCT373566 is a potent and orally active degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo[1].
Dynasore is a cell-permeable dynamin inhibitor with an IC50 of 15 μM.
6-O-Feruloylglucose is a natural product that exhibits antioxidant activity[1][2].
Amino-PEG5-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].