DDX3-IN-2 is an active DEADbox polypeptide 3 (DDX3) inhibitor with an IC50 value of 0.3 μM. DDX3-IN-2 shows a broad spectrum of antiviral activity. DDX3-IN-2 has the potential to overcome HIV resistance[1].
Flumorph(SYP-L190) is a carboxylic acid amide (CAA) fungicide.IC50 value:Target: Fungicide agentFlumorph did not inhibit the synthesis of cell wall materials, but disturbed the polar deposition of newly synthesized cell wall materials during cystospore germination and hyphal growth. In flumorph-treated hyphae, the most characteristic change was the development of periodic swelling ("beaded" morphology) and the disruption of tip growth. Upon removing flumorph, normal tip growth and organized F-actin were observed again [1]. Flumorph had induced systemic genotoxicity in mammals as it caused DNA damage in all tested vital organs, especially in brain and spleen [2].
KKL-35 is a trans-translation tagging reaction inhibitor with an IC50 of 0.9 µM.
Cefathiamidine is a first-generation cephalosporin antibacterial agent and is used to treat infections caused by susceptible bacteria. Cefathiamidine exhibits a wide spectrum of antimicrobial activity against bacteria. Cefathiamidine is used for the treatment of respiratory, liver, five senses, urinary tract infections, endocarditis and sepsis[1][2].
Stearyl gallate is an alkyl gallate with a long alkyl chain (carbon number of 18). Stearyl gallate has an antioxidant activity, and a weak antiviral activity against HSV-1[1][2].
Dodicin hydrochloride is an effective disinfectant with broad antimicrobial activity[1].
Picloxydine is a heterocyclic biguanide with antibacterial and antiplaque activity.
Antifungal agent 53 (A03) is a potent inhibitor of Candida albicans CYP51 with antifungal activity. Antifungal agent 53 prevents the formation of fungi biofilms. Antifungal agent 53 also exhibits good safety[1].
4-Hydroxyoxyphenbutazone kills both replicating and nonreplicating (NR) Mycobacterium tuberculosis (Mtb), including Mtb resistant to standard drugs. 4-Hydroxyoxyphenbutazone is a potent inhibitor of cytokine production. 4-Hydroxyoxyphenbutazone is an immunosuppressive drug and has the potential for rheumatoid arthritis research[1][2].
Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities[1][2][3].
Myristoyl glutamic acid sodium is a common ingredient in cosmetics/creams. Myristoyl glutamic acid sodium, a surfactant belonging to the amino acid, has mild cleaning properties and is also foamy and mildly bacteriostatic[1].
Ethambutol-d8 is deuterium labeled Ethambutol.
2-Methoxybenzaldehyde (o-Anisaldehyde), isolated from cinnamon essential oil (CEO), exists antibacterial and antifungal activity[1].
Thymol-d13 is the deuterium labeled Thymol[1]. Thymol is the main monoterpene phenol occurring in essential oils isolated from plants belonging to the Lamiaceae family, and other plants such as those belonging to the Verbenaceae, Scrophulariaceae, Ranunculaceae and Apiaceae families. Thymol has antioxidant, anti-inflammatory, antibacterial and antifungal effects[2].
2'-C-Methyladenosine is an inhibitor of hepatitis C virus (HCV) replication. 2'-C-Methyladenosine inhibits HCV replicon and NS5B-catalyzed RNA synthesis with IC50 values of 0.3μM and 1.9 μM, respectively. 2'-C-Methyladenosine also potently inhibits LRV1 in Leishmania guyanensis (Lgy) and Leishmania braziliensis[1][2].
N-Decyl-N,N-dimethyldecan-1-aminium chloride (Didecyldimethylammonium chloride) is a dialkyl-quaternary ammonium compound that is used in numerous products for its bactericidal, virucidal and fungicidal properties[1].
Piperonyl butoxide is a semisynthetic derivative of safrole，used as a component of pesticide formulations. It is a synergist, despite having no pesticidal activity of its own, it enhances the potency of certain pesticides such as Carbamates, Pyrethrins, Pyrethroids, and Rotenone.
Fluconazole (mesylate) is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.Target: AntifungalFluconazole (mesylate) is the mesylate salt form of fluconazole, which is a triazole antifungal intended for oral treatment of superficial and systemic mycoses. In tests done in standard mycological media, the compound had minimal inhibitory concentrations against pathogenic Candida species that were usually in excess of 100 mg/l. Fluconazole inhibited branching and hyphal development in C. albicans at concentrations as low as 10(-6) M (0.3 mg/l), but miconazole and ketoconazole were still active in these tests at concentrations 100 times lower than this [1]. Oral fluconazole was not associated with a significantly increased risk of birth defects overall or of 14 of the 15 specific birth defects of previous concern. Fluconazole exposure may confer an increased risk of tetralogy of Fallot [2]. Fluconazole is predicted to be ineffective against Cryptococcus gattii in the koala as a sole therapeutic agent administered at 10 mg/kg p.o. every 12 h [3].Clinical indications: Balanitis; Candida infection; Cryptococcus infection; Cryptococcus neoformans meningitis; Dermatomycosis; Female genital tract infection; Fungal infection; Fungal respiratory tract infection; Fungal urinary tract infection; Prophylaxis; Tinea capitis; Tinea corporis; Tinea cruris; Tinea pedis .Toxicity: Symptoms of overdose include hallucinations and paranoid behavior.
Itraconazole-d3 (R51211-d3) is the deuterium labeled Itraconazole (HY-17514)[1].
α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation.
Kanamycins sulfate is a broad-spectrum antibiotic, can be used in certain severe staphylococcal or Gram-negative bacillary infections. Kanamycin sulfate has certain ototoxicity[1][2].
Colistin methanesulfonate sodium salt exhibits MIC values ranged from 4 to 16 mg/liter against susceptible strains (P. aeruginosa)[1].
HSGN-94 is a potent antimicrobial agent with lipoteichoic acid (LTA) biosynthesis inhibition. HSGN-94 inhibits drug-resistant Gram-positive bacteria with MIC values of 0.25-2 μg/mL. HSGN-94 inhibits biofilm formation of MRSA and Vancomycin-resistant Enterococci. HSGN-94 also inhibits pro-inflammatory cytokines, exhibits in vivo efficacy in an MRSA murine wound infection model[1].
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
Tulathromycin A is a macrolide antibiotic.IC50 Value: 1 microg/ml (MIC90 for Pasteurella multocida) [2]Target: Antibacterialin vitro: Two highly pathogenic strains of M. bovis (with minimum inhibitory concentration values for tulathromycin of 1 and >64 microg/ml) were inoculated into 145 calves. Four days after inoculation, calves with clinical BRD were treated subcutaneously with saline or tulathromycin (2.5 mg/kg). Compared with saline, BRD-related withdrawals, peak rectal temperatures, and lung lesion scores were significantly lower for tulathromycin-treated calves (P < .01). Tulathromycin was highly effective in the treatment of BRD due to M. bovis in calves regardless of the minimum inhibitory concentration of the challenge strain (1 or >64 microg/ml) [1]. The lowest concentrations inhibiting the growth of 90% of isolates (MIC90) for tulathromycin were 2 microg/ml for Mannheimia (Pasteurella) haemolytica, 1 microg/ml for Pasteurella multocida (bovine), and 2 microg/ml for Pasteurella multocida (porcine) and ranged from 0.5 to 4 microg/ml for Histophilus somni (Haemophilus somnus) and from 4 to 16 microg/ml for Actinobacillus pleuropneumoniae [2]. in vivo: Each study randomly allocated 250 calves to receivetulathromycin at 2.5 mg/kg and 250 calves to receive either tilmicosin at 10 mg/kg (Colorado site) or florfenicol at 40 mg/kg (Idaho and Texas sites) on arrival at the feedlot. Calves were housed by treatment group in pens with 50 calves/pen [3]. The treatment groups were physiologic saline (n = 160) given SC at 0.02 ml/kg, tulathromycin (n = 320) given SC at 2.5 mg/kg, and tilmicosin (n = 320) given SC at 10 mg/kg [4].Tulathromycin is a triamilide antimicrobial that has been approved for use in the treatment and prevention of bovine respiratory disease and the treatment of swine respiratory disease. Toxicity: No adverse events related to tulathromycin were reported [4].Clinical trial:
Diethofencarb is a fungicide with strong activity against Botrytis cinerea and Benzimidazole-resistant strains of Botryis spp. Diethofencarb has a role as an antifungal agrochemical[1].
Maximin 8 is a antimicrobial peptide that can be found in B. maxima[1].
UM729 is a new pyrimidoindole, which has an additive effect with AhR antagonists in preventing differentiation in most AML specimens; collaborates with Ahr suppressors in preventing AML cell differentiation.IC50 value:Target: SR1 and UM729 can be implemented as a standardized supplement in culture media and will pave the way for studies of self-renewal mechanisms and for the identification of new antileukemic drugs through cell-based assays for primary human AML cells.
Lugdunin is an antibiotic peptide. Lugdunin inhibits bacteria by dissipating their membrane potential. Lugdunin is active against Gram-positive bacteria, such as S. aureus, and reduces S. aureus skin and nasal colonization. Lugdunin induces LL-37 and CXCL8/MIP-2 in human keratinocytes and mouse skin[1].
Kushenol W is a prenylated flavonoid that can be isolated from the root of Sophora flavescens. Kushenol W has antimicrobial effect, with a MIC of 10 μg/mL for Staphylococcus aureus[1].