dc 1

DC1 can be used to synthesize antibody-drug conjugates targeted to the treatment of cancer, is an ADC cytotoxin, similar to the small groove-binding DNA alkylating agent CC-1065.

AntibioticDC 102 is a novel glycosylated pyrrole (1,4) benzodiazepine-class antibiotic targeting Bacillus subtilis, with a minimum inhibitory concentration (MIC) of 42 μg/mL. The lethal dose 50 (LD50) in mice, when administered intraperitoneally (i.p), is 1.5 mg/mL.

SJ6986 is a potent, selective, and orally active GSPT1/2 degrader, effectively degrading GSPT1 with a DC50 of 2.1 nM (D max 99%) [1].

DC-05 is an inhibitor of DNA methyltransferase 1 (DNMT1) (IC50 and a Kd: 10.3 μM and 1.09 μM, respectively).

PROTAC FGFR2 degrader 1 (compound N5) is a potent PROTAC that efficiently targets FGFR2, boasting a DC 50 value of 6.46 nM and an FGFR2 IC 50 of 0.08 nM. This compound exhibits significant anti-proliferative effects and high selectivity. It induces G0/G1 arrest in the cell cycles of KATOIII and SNU16 and inhibits apoptosis by diminishing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. Additionally, PROTAC FGFR2 degrader 1 maintains over 50% inhibition of gastric cancer cells at a concentration of 0.17 nM and effectively suppresses the growth of SNU16 xenograft tumors in a mouse model.

DMT-dC(bz) Phosphoramidite is commonly employed in the synthesis of DNA [1].

5'-O-DMT-N4-Ac-dC (N4-Acetyl-2'-deoxy-5'-O-DMT-cytidine, compound 7) is a deoxynucleoside used in synthesizing dodecyl phosphoramidite, a crucial precursor for dod-DNA production. Dod-DNA is amphiphilic DNA with dodecyl phosphotriester linkages, featuring an internal hydrophobic region[1][2].

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.

DC661 is a palmitoyl-protein thioesterase 1 (PPT1) inhibitor that acts as an anti-lysosomal agent by inhibiting autophagy, demonstrating anti-cancer activity.

1. Nitidine chloride has inhibitory effects on various tumors, such as renal cancer , breast cancer. 2. Nitidine chloride inhibits the proliferation of SMMC-7721 cells in vitro in a time- and dose-dependent manner and identifies efficacy in vivo in a mouse model of HCC.

DC-CPin7, a powerful inhibitor of the bromodomain of CREB-binding protein (CBP), exhibits an IC50 value of 2.5 μM [1].

DC-CPin711, a potent and selective inhibitor of the bromodomain of CREB-binding protein (CBP) with an IC50 of 0.0626 μM, effectively halts the cell cycle at the G1 phase and promotes apoptosis [1].

DC-LC3in-D5 is a potent and selective covalent inhibitor of LC3A/B that disrupts autophagy by covalently binding to Lys49 on LC3B (IC₅₀ = 200 nM), resulting in impaired LC3B lipidation, accumulation of the autophagy substrate p62, and a significant reduction in the formation of autophagosome vesicles.

IRAK4-IN-18 is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK4) (IC50: 15 nM). It inhibits LPS-induced IL23 production in THP and DC cells and blocks the development of arthritis in rats, making it useful for studying arthritic diseases.

HPK1-IN-29 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), a negative regulator of the activation response of dendritic cells (DCs), T cells, and B cells. HPK1-IN-29 enhances anti-tumor immunity in humans and shows potential for studying immune-related diseases, particularly tumors.

IRAK4-IN-19 is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK4) with an IC50 of 4.3 nM. It inhibits LPS-induced IL23 production in THP and DC cells and suppresses arthritis development in arthritic model rats. IRAK4-IN-19 can be used to study arthritic diseases.

HPK1-IN-28, a potent inhibitor of HPK1, enhances anti-tumor immunity in humans and demonstrates research potential in immune-related diseases, particularly tumors, by acting as a negative regulator of dendritic cell (DC), T-cell, and B-cell activation responses.

DNMT3A-IN-1 is a selective and potent DNMT3A inhibitor. DNMT3A-IN-1 exhibits inhibitory activity against DNMT3A with a KI ranging from 9.16-18.85 μM (AdoMet) and 11.37-23.34 μM (poly dI-dC).

DC 015 is a novel potent and selective alpha 1-adrenoceptor antagonist.

Antibiotic DC 81, a pyrrolo[2,1-c][1,4]benzodiazepine (PBD) antitumor antibiotic produced by Streptomyces species, acts as a potent inhibitor of nucleic acid synthesis. It specifically recognizes and binds to certain DNA sequences, forming a labile covalent adduct [1] [2].

KTX-951, a PROTAC designed for IRAK4 degradation (DC 50 =18 nM), exhibits an oral bioavailability (F%) of 22% in a rat model at a dosage of 10 mg/kg. Additionally, KTX-951 demonstrates promising anticancer potential [1].

AK-2292 is a potent and selective STAT5 PROTAC degrader with a DC50 of 0.10 μM. It induces degradation of STAT5A/B proteins in vitro and in vivo and can cause tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models [1] [2].

PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080 cells [1].

PROTAC pan-IAP degrader-1 (Compound 9) is a pan- IAP degrader PROTAC . PROTAC pan-IAP degrader-1 degrades XIAP , cIAP1 and cIAP2 with DC 50 s of 0.7, 2.4, and 6.2 nM in MM.1S cells, respectively [1] .