Zosuquidar trihydrochloride is an inhibitor of P-glycoprotein with a Ki value of 59 nM.
4′-Bromoflavone, a cancer chemopreventive agent, is a potent phase II detoxification enzymes inducer[1].
2’-Chloro-N6-benzyl adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Norathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM[1]. Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively[2]. Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 is a Drug-Linker Conjugate for ADC. SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 consists of the anti-cancer agent SN38 (HY-13704) and a linker Lys(MMT)-PAB-oxydiacetamide-PEG8-N3 (HY-131157). SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 can be used for synthesis of ADCs[1].
Val-Cit-PAB-OSBT GMP is a GMP grade Val-Cit-PAB-OSBT (HY-78736). Val-Cit-PAB-OSBT is a degradable ADC linker, which is composed of the polypeptide Val-Cit-PAB and OSBT groups coupled together[1].
Tebentafusp (IMCgp100) is a bispecific fusion protein to target gp100 peptide-HLA-A*02:01 (a melanoma-associated antigen). Tebentafusp guides T cells to kill gp100-expressing tumor cells via a high affinity T-cell receptor (TCR) binding domain and an anti-CD3 T-cell engaging domain. Tebentafusp leads to inflammatory cytokines and cytolytic proteins production, resulting in the direct lysis of tumour cells[1][2].
5′-O-[(4-Cyanophenyl)methyl]-2′,3′-O-(1-methylethylidene)adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Adenine hydrochloride (6-Aminopurine hydrochloride) is a purine derivative with a variety of roles in biochemistry, including cellular respiration, in the form of both the energy-rich adenosine triphosphate (ATP) and the cofactors nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD), and protein synthesis, as a chemical component of DNA and RNA[1][2].
Di-N-desethyl Amiodarone hydrochloride is a metabolite of Amiodarone (HY-14187). Di-N-desethyl Amiodarone hydrochloride is a strong inhibitor of the respiratory chain[1].
PRMT5-IN-9 is a novel PRMT5 inhibitor for treating cancer, with an IC50 of 0.01 μM.
GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer’s disease, Parkinson’s disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.
2’,3’-Bis(O-t-butyldimethylsilyl)-4’,5’-didehydro-5’-deoxyuridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
5-Hydroxy-arabinouridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
TCO-GK-PEG4-NHS ester is an ADC Linker, and can be used for synthesis of [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d. [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d binds with high affinity and immunoreactivity to HER2[1].
Cecropin A is a linear 37-residue antimicrobial polypeptide, with anticancer and anti-inflammatory activity.
DB1976 is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 has apoptosis-inducing effect[1][2][3].
ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER), with an DC50 of 0.17 nM in MCF-7 cells[1].
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy[1].
TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
Coumarin is the primary bioactive ingredient in Radix Glehniae, named Beishashen in China, which possesses many pharmacological activities, including anticancer, anti-inflammation and antivirus activities.
RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells[1].
JPH203 Dihydrochloride is a tyrosine analog, acts as a selective inhibitor of L-type amino acid transporter 1 (LAT1), and is used in cancer research.
BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes[1].
PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
Miroestrol is a highly active phytoestrogen. Miroestrol can produce mammogenic effect. Miroestrol exhibits bone loss prevention and neuroprotective in ovariectomized mice. Miroestrol also can reduce cancer risk[1][2][3][4].
HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin[1].
3-O-Benzoyl-1,2: 5,6-bis(di-O-isopropylidene)-alpha-D-galactofuranose is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. IC50 value:Target: sigma-2 receptor; lysosome-destabilizing agentsiramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was rapidly lost [1]. Siramesine, a sigma-2 receptor agonist originally developed as an anti-depressant, can induce cell death in transformed cells through a mechanism involving lysosomal destabilization [2].in vivo: SA4503 or siramesine given jointly with MEM (as well as with AMA) decreased the immobility time in rats. The effect of SA4503 and AMA co-administration was antagonized by progesterone, a sigma1 receptor antagonistic neurosteroid. Combined treatment with siramesine and AMA was modified by neither progesterone nor BD1047 (a novel sigma antagonist with preferential affinity for sigma1 sites) [3]