K67 is a specific inhibitor of the interaction between S349-phosphorylated p62 and Keap1, exhibts no inhibitory effect on the interaction of full-length Keap1 with Nrf2-ETGE or full-length Nrf2; has specific inhibitory effect on the Nrf2 target genes, dramatically suppresses the proliferations of Huh1 cells and of Huh7 cells expressing phospho-mimetic p62.
6a-Hydroxymedicarpin is a monoterpenoid indole alkaloid that can be isolated from Ochrosia elliptica. 6a-Hydroxymedicarpin has anticancer activity[1].
Phenyl β-D-glucopyranoside has anti-cancer and anti-inflammatory activities. Phenyl β-D-glucopyranoside inhibits nitric oxide (NO) production, and the expression of iNOS and COX-2. Phenyl β-D-glucopyranoside also inhibits the nuclear translocation of NF-κB[1].
6-Deoxyisojacareubin is a PKC inhibitor that inhibits the proliferation of QGY-7703 cells in a concentration-dependent manner. 6-Deoxyisojacareubin is also a natural product that can be obtained from Garcinia nervosa. 6-Deoxyisojacareubin can be used in cancer research[1].
Deltarasin is an inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Sabarubicin is a doxorubicin disaccharide analogue with striking antitumor activity. Sabarubicin is more effective than doxorubicin as a topoisomerase II poison and stimulated DNA fragmentation at lower intracellular concentrations.
PROTAC FAK degrader 1 is a selective and potent focal adhesion kinase (Fak) degrader with an IC50 of 6.5 nM, DC50 of 3 nM[1].
HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA)[1].
MZ 1 is a BRD4 protein degrader based on PROTAC technology.
K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase[1][2][3].
XZH-5 is a small moelcule that inhibits constitutive and interleukin-6-induced STAT3 phosphorylation, inhibits STAT3 DNA binding ability and downregulation of STAT3 downstream genes; inhibits downregulation of STAT3 downstream genes, such as Bcl-2, Bcl-xL, Cyclin D1 and Survivin, demonstrates blockade of STAT3 phosphorylation in human rhabdomyosarcoma cells with apoptosis and suppresses colony-forming ability and cell migration; blocks IL-6-induced STAT3 phosphorylation and nuclear translocation but not the stimulation of STAT1 phosphorylation by IFN-γ.
L-Lysine-15N (dihydrochloride) is a 15N-labeled Deruxtecan. Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and amaleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
4′-C-2-Propen-1-yluridine 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].
dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1[1].
L-Ascorbic acid-d2 is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla
N6-Dimethylaminomethylidene isoguanosine 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].
Alda-1 is a potent ALDH2 agonist, which activates wild-type ALDH2 and restores near wild-type activity to ALDH2*2.
PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC50 of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research[1].
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).Target: GnRHin vitro: Elagolix is a short-acting, nonpeptide, GnRH antagonist, administered orally, that unlike injectable depot GnRH agonists and antagonists, produces a dose-dependent suppression of ovarian estrogen production, that is, from partial suppression at lower doses to full suppression at higher doses. Elagolix is regarded as the frontrunner of a new class of GnRH inhibitors that have been denoted as second-generation, due to their non-peptide nature and oral bioavailability.
Gefitinib D8 (ZD1839 D8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells[1][2].
HDAC8-IN-3 (compound P19) is a potent HDAC8 inhibitor with IC50 value of 9.3 μM and produces thermal stabilization. HDAC8-IN-3 has cytotoxicity and induces apoptosis in leukemic cell lines[1].
EGGGG-PEG8-amide-bis(deoxyglucitol) is a cleavable ADC linker.
XIAP BIR2/BIR2-3 inhibitor-1 (compound 3) is a dual inhibitor of BIR2 and BIR2-3 with IC50s of 1.9 and 0.8 nM, respectively. XIAP BIR2/BIR2-3 inhibitor-1 can used in study cancers[1].
Mal-PEG2-VCP-Eribulin consists the ADCs linker (Mal-PEG2-VCP) and Eribulin[1]. Eribulin is a mechanistically unique microtubule inhibitor for cancer[2]. Mal-PEG2-VCP-Eribulin is an Eribulin-based drug for antibody conjugates[1].
HDAC-IN-50 is a potent and orally active Apoptosis<0/b> and Apoptosis<1/b> dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1,>Apoptosis<2 pSTAT3. HDAC-IN-50 shows anti-tumor activity[1].
Dihydroprehelminthosporol (Compound 1) from the fungusVeronaea sp.of the separated. Dihydroprehelminthosporol on human cancer cell line A549 and SK-0A-3 has cytotoxicity[1].
Tinurilimab (Bay 1834942) is an anti-CEACAM6 monoclonal antibody. CEACAM6 is an immune checkpoint regulator suppressing the activity of effector T-cells against tumors[1].
mPEG-amine (MW 3400) can synthesize folate-conjugated polymer micelles for encapsulation of anticancer agent 9-nitrocamptothecin (HY-16560). folate-conjugated polymer micelles are effective carriers of insoluble anticancer drugs, which can avoid macrophages and play a role in endocytosis of tumor cells mediated by folate receptors (FR).
Campesterol is a plant sterol with cholesterol lowering and anticarcinogenic effects.
Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM[1], and also inhibits ACE-I activity[2]. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells[1]. Sinapinic acid shows antioxidant and antidiabetic activities[2]. Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats[3].