dc-1

TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity. It effectively hinders the transition from trophozoite to schizont, impairs transcription, and diminishes transmission to the mosquito vector.

ADC-13 is a bioactive chemical agent.

TCMDC-135051 TFA is a highly selective and potent inhibitor of protein kinase PfCLK3.

DC-159a, an 8-methoxy fluoroquinolone, possesses broad-spectrum antibacterial activity, with a particular efficacy against Gram-positive pathogens. The MIC90 values for DC-159a are 0.5 μg mL against Streptococcus anginosus group, 4 μg mL against Clostridium difficile, and 2 μg mL against Bacteroides fragilis.

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4 nM, 2.4 nM, and 15.7 nM, respectively.

TCMDC-125457 can effectively induce calcium redistribution, but has little effect on inhibiting heme crystallization. When TCMDC-125457 is combined with artesunate, it can effectively treat tightly synchronized artemisinin-resistant ring-stage parasites.

TCMDC-125431 is a novel inhibitor of Plasmodium calcium kinetics with minimal inhibition of haemoglobin crystals.

TCMDC-136230 is a novel inhibitor of Plasmodium calcium kinetics with minimal inhibition of haemoglobin crystallisation.

TCMDC-135051 hydrochloride is a potent, highly selective, low off-target toxicity inhibitor of the protein kinase PfCLK3. TCMDC-135051 hydrochloride blocks the trophozoite to lysosome transition, disrupts transcription and inhibits transmission to mosquito vectors, exhibiting an antiparasitic effect with an EC50 value of 320 nM.

TCMDC-135051 TFA is a potent, highly selective, low off-target toxicity protein kinase PfCLK3 inhibitor that exhibits antiparasitic effects with an EC50 value of 320 nM. TCMDC-135051 TFA blocks the trophozoite to lytic transition, disrupts transcription and inhibits transmission to mosquito vectors.

DC-120 is an ATP competitive AKT kinase inhibitor that suppressed proliferation and induced apoptosis in liver cancer cells both in vitro and in vivo. DC120 blocked the phosphorylation of downstream molecules in the AKT signal pathway in dose- and time-dependent manners both in vitro and in vivo. DC120 inhibits AKT activity in vitro with an EC(50) of 153 nM. DC120 at 20 mg kg day inhibited the CNE2 xenograft tumor growth with a treated group control group ratio of 38.1%, accompanied by increasing terminal deoxynucleotidyl transferasedUTP nick-end labeling-positive cells in the tumor sample.

BKIDC-1553, an orally active antiglycolytic agent and bumped kinase inhibitor-derived compound, has a predicted half-life of approximately 17 hours in humans. It inhibits CYP2C8 and Angiotensin Converting Enzyme, making it suitable for cancer research [1].

TCMDC-137332 is a compound exhibiting antimalarial activity against Plasmodium falciparum with an IC50 value of 7 nM, and can be utilized for malaria research [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.

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].

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

Glutathione synthesis-IN-1 (DC-1) is an inhibitor of glutathione synthesis[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.

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].