inh-1

ODN INH-1, a palindromic and class R ('restricted') inhibitory ODN, is a potent inhibitor of TLR9-induced B cells and macrophages.

INH1 (IBT13131) is a cell-permeable Hec1 inhibitor that specifically disrupts the Hec1/Nek2 interaction.

INH-13 is a Aurora inhibitor.

T3Inh-1 is a potent and selective ppGalNAc-T3 inhibitor with IC50 of 7 µM. T3Inh-1 protects against breast cancer cells. T3Inh-1 reduces FGF23 hormone levels in tissue cells and mice without causing any toxic side effects.

4-aminobenzoic acid is an organic acid with UV-absorbing and antifibrotic properties. When exposed to light, 4-aminobenzoic acid absorbs UV light and releases excess energy through a photochemical reaction, which may cause DNA damage.4-aminobenzoic acid also increases oxygen uptake at the tissue level and may enhance monoamine oxidase (MAO) activity to promote serotonin degradation, which in excess may lead to fibrotic Changes.

INH154 is a highly potent inhibitor of Nek2 and Hec1 binding (INH), with IC50 values of 120 nM in MB468 cells and 200 nM in Hela cells.

Ajugamarin H1 is a natural product that can be used as a reference standard.

4-Aminobenzoic acid (PABA) potassium is a modulator of catecholamine oxidation reactions. It holds promise for research in Parkinson's disease and hypertension.

CFTR(inh)-172 (CFTR Inhibitor-172) is a voltage-independent, selective CFTR inhibitor.

Prostaglandin H1 is the cyclooxygenase metabolite of DGLA, a CRTh2 agonist and a precursor of a family of 1 anti-inflammatory prostaglandins. Prostaglandin H1 can be used in the study of inflammation.

INH14 is a novel inhibitor of the IKKα/β-dependent TLR inflammatory response (IC50s: 8.97/3.59 μM for IKKα/IKKβ).

Sanguiin h 11 is a compound purified from the plant Sanguisorba officinalis and has proven to be a potent inhibitor of chemoattractant-dependent and independent neutrophil movement.

MK-8712 is a monobactam beta-lactamase inhibitor.

Maximin H1, an antimicrobial peptide sourced from the skin secretions of the Chinese red belly toad (Bombina maxima), exhibits efficacy against several pathogens, including Escherichia coli (ATCC25922), Staphylococcus aureus (ATCC2592), Bacillus pyocyaneus (CMCCB1010), and Candida albicans (ATCC2002). Corresponding minimum inhibitory concentration (MIC) values are 9, 4.5, 9, and 4.5 μg/ml, respectively [1].

Bombinin H1, an antimicrobial peptide originating from the skin of the Bombina variegata moth, exhibits lethal concentrations of 3.8 μM against Escherichia coli D21 and 2.1 μM against Staphylococcus aureus Cowan 1 [1].

Biotin-H10 is a potent inhibitor of anterior gradient homolog 2 (AGR2) with a dissociation constant (K_D) of 6.4 nM, effectively reducing the viability of cancer cells [1].

Monamycin H1 is an ester peptide antibiotic that exhibits activity against Gram-positive bacteria.

RNF5 agonist 1 (analog-1), a structural analog of the RNF5 inhibitor inh-02, is a potent RNF5 agonist. In CFBE41o- cells expressing F508del-CFTR, RNF5 agonist 1 enhances the ubiquitination of ATG4B.

RNF5 inhibitor inh-02 is a selective inhibitor of the ubiquitin ligase RNF5/RMA1, which can significantly rescue F508del-CFTR (cystic fibrosis transmembrane conductance regulator with a deletion at position 508 of phenylalanine) and regulate ATG4B and paxillin, making it useful for studying cystic fibrosis (CF).

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg/ml) and Kurono (MIC: 0.0005 μg/ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg/ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg/ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg/ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg/kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1/2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg/kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg/kg to 2.5 mg/kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg/kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.

Thiocarlide (isoxyl) is a thiourea derivative that was used in the 1960s to successfully treat tuberculosis (TB). It has considerable antimycobacterial activity in vitro and is effective against multi-drug resistant strains of Mycobacterium tuberculosis in the range of 1-10 µg/ml. [1] [2] At concentrations of 10 µM, isoxyl inhibits the synthesis of M. bovis during six hours of exposure which is similar to isoniazid (INH) and ethionamide (ETH), two other predominant anti-tuberculosis drugs. Unlike INH and ETH, isoxyl also partially inhibits the synthesis of fatty acids. Isoxyl shows no acute toxicity against primary macrophage cell cultures as demonstrated by diminution of redox activity.[2]

Mtb-IN-4 (compound 17h) is a non-toxic isoxazole that exhibits anti-Mycobacterium tuberculosis (Mtb) activity with an IC50 value of 0.70 μM. It impedes Mtb respiration and biofilm formation within macrophages and augments the efficacy of the antibiotic isoniazid (INH) against INH-resistant Mtb mutants [1].

Mtb-IN-5 (compound (-)17j) is an isoxazole with anti-Mycobacterium tuberculosis (Mtb) activity, inhibiting Mtb respiration and biofilm formation within macrophages, and enhancing the efficacy of the antibiotic isoniazid (INH) against INH-resistant Mtb mutants [1].