CC-17369 (7-Hydroxy pomalidomide) is a metabolite of Pomalidomide. CC-17369 is the Pomalidomide -based cereblon (CRBN) ligand used in the recruitment of CRBN protein. CC-17369 can be connected to the ligand for protein by a linker to form PROTAC[1].
Calcium Orange AM is an intracellular calcium reporter. Specific fluorescence can be detected when free calcium binds to Calcium Orange AM (Ex/Em=549/576 nm). Calcium Orange AM does not enter the vacuoles and does not compartmentalize into acidic vesicles[1].
Thalidomide-O-C6-NHBoc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
MAHMA NONOate is a NO donor. MAHMA NONOate effectively inhibits platelet aggregation induced by either collagen or ADP[1].
m-PEG7-CH2COOH is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Emodin is a broad-spectrum anticancer agent. Emodin inhibits casein kinase II (CKII) activity with IC50 of 2 μM.
Acetyl octapeptide-1 is a bioactive peptide with anti-wrinkle effect and has been reported used as a cosmetic ingredient[1].
4-Nitrocatechol is a potent lipoxygenase inhibitor[1].
Toremifene (NK 622; FC 1157a) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.IC50 Value: 1±0.3 μMTarget: Estrogen receptorToremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis and other adverse effects resulting from ADT in men with prostate cancer [1]. in vitro: The growth of Ac-1 cells was inhibited by tamoxifen, toremifene and atamestane in vitro with IC50values of 1.8±1.3μM, 1±0.3μM and 60.4±17.2μM, respectively. The combination of toremifene plusatamestane was found to be better than toremifene or atamestane alone in vitro[2].in vivo: The effect of this combination was then studied in vivo using Ac-1 xenografts grown in ovariectomized female SCID mice. The mice were injected with toremifene (1000μg/day), atamestane (1000μg/day), tamoxifen (100μg/day), or the combination of toremifene plus atamestane. In this study, our results indicate that the combination of toremifene plus atamestane was as effective as toremifene or tamoxifen alone but may not provide any additional benefit over toremifene alone or tamoxifen alone[2].Clinical trail: Prostate cancer diagnosis among men with isolated high-grade intraepithelial neoplasia enrolled onto a 3-year prospective phase III clinical trial of oral toremifene[3].
Salinomycin sodium salt is an anticoccidial drug with potent anti-bacterial activity and an novel anticancer agent targeting human cancer stem cells.
Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity[1][2].
Phrixotoxin 1, from the venom of the theraphosid spider Phrixotrichus auratus, is a specific peptide inhibitor of Kv4 potassium channel[1][2].
Anticancer agent 96 (Compound 4) is an anticancer agent that shows cytotoxic activities against human cancer cells[1].
Epimedin B, a component extracted from Epimedii Folium, is reported to have antiosteoporotic activity.IC50 value:Target:In vitro:In vivo: Prednisolone-induced osteoporosis model using zebrafish was used to evaluate the antiosteoporotic activity of micro amount epimedin B. The result showed that 1 μmol·L- 1epimedin B groups were significantly increased when compared with model group; Epimedin B can prevent zebrafish osteoporosis induced by prednisolone [1].
Oroxylin 7-O-glucoside is a flavone. Oroxylin 7-O-glucoside can be isolated from? hot methanol extracts of? Scutellaria ouata[1].
ZZW-115 (ZZW115, ZZW 115) is a potent inhibitor of NUPR1 (Kd=2.1 uM), an intrinsically disordered protein (IDP) with an entirely disordered conformation; demonstrates antitumor activity on a panel of 11 primary PDAC-derived cells and it was found to be efficient to kill the cancer cells with IC50 in the range from 0.84 μM (ANOR) to 4.93 μM (HN14), also inhibits the growth of other tumors-derived cells (IC50=0.42 μM (Hep2G cells) to 7.75 μM (SaO-2 cells)); induces pancreatic cell death by necrosis and apoptosis and inhibits the growth pancreatic xenografted tumors in vivo.
MK-0952 is a selective and orally active PDE4 inhibitor, with an IC50 of 0.53 nM. MK-0952 has the potential for Alzheimer’s disease study[1][2].
DMNPE-4 AM-caged-calcium, photolabile analogues of EGTA, is an extremely effective Ca2+ selective cage, with a Kd for Ca2+ of 48 nM and 19 nM at pH 7.2 and pH 7.4, respectively. DMNPE-4 AM-caged-calcium has a lower affinity for Ca2+ (Kd=~2 nM) after photolysis[1][2].
PI3K-IN-20 is a PI3k inhibitor extracted from WO2017101847 A1, compound 1[1].
4'-Methylacetophenone-d10 is the deuterium labeled 4'-Methylacetophenone[1]. 4′-methylacetophenone can be used as a fragrance material. 4′-Methylacetophenone is wildly occurs in volatile compounds in food and in some natural complex substances (NCS)[2].
MMAF intermediate 2 is an intermediate for the synthesis of MMAF (HY-15579). MMAF (Monomethylauristatin F) is a potent inhibitor of tubulin polymerization and the cytotoxic (ADC Cytotoxin) component of classic antibody drug conjugates (ADCs), such as Vorsetuzumab mafodotin and SGN-CD19A[1].
BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research[1].
Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase)[1].
m-PEG3-Boc is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs[1].
Cholecalciferol(Vitamin D3) is a naturally occuring form of vitamin D; Reported that upon metabolic activation, Cholecalciferol induces cell differentiation and prevents proliferation of cancer cells. IC50 value:Target: Vitamin D acts through a receptor that is a member of the ligand-dependent transcription factor superfamily. Modulates the proliferation and differentiation of both normal and cancer cells. Has antiproliferative and antimetastatic effects on breast, colon, and prostate cancer cells. Activated vitamin D receptors in intestine and bone maintain calcium absorbance and homeostasis.
D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods.
Ranibizumab (RG-6321) (anti-VEGF) is a humanized anti-VEGF monoclonal antibody fragment and can recognize all VEGF-A isoforms (VEGF110, VEGF121, and VEGF165)[1]. Ranibizumab (anti-VEGF) slows vision loss in vivo and is used for wet age-related macular degeneration (AMD) research[1].
4’-Methylguanosine is a purine nucleoside analogue. 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].
ML298 is a potent, selective phospholipase PLD2 inhibitor with IC50 of 355 nM, displays >53-fold selectivity over PLD1 (IC50>20 uM); decreases invasive migration in U87-MG glioblastoma cells; has an attractive DMPK profile, making it an attractive tool compound to further dissect PLD2 function in multiple cellular and in vivo environments.
Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.