Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis[1][2].
Bis-propargyl-PEG4 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG4 is used for the synthesis of demethylvancomycin dimers[1][2].
Trilaciclib hydrochloride is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
Eicosanedioic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Eicosanedioic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis
Alisertib (MLN 8237) is a selective Aurora A inhibitor with an IC50 of 1.2 nM.
KLK7/ELA2-IN-1 is a potent kallikrein-related peptidase 7 (KLK7) and epidermal elastase 2 (ELA2) inhibitor with IC50s of 6 nM and 55 nM, respectively (WO2009024527A1, Example 4)[1].
TBK1-IKKε inhibitor II is a potent, selective dual inhibitor of TBK1/IKKε with IC50 of 13 nM/59 nM, respectively; displays 100- to 1000-fold less activity against other tested protein kinases including PDK1, PI3K family members and mTOR; inhibits LPS-induced expression of IFNβ (IC50=62 nM), and the IFNβ target genes IP10 (IC50=78 nM) and Mx1 (IC50=20 nM); effectively blocks TLR3-dependent IRF3 nuclear translocation in cells with IC50<100 nM.
3’,5’-Di-O-acetylthymidine 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].
Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM.
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1].
9-Aminocamptothecin is a topoisomerase I inhibitor with potent anticancer activity.
PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, 100-fold selectivity versus Chk2 (Ki, 47 nM).
(R)-Casopitant ((R)-GW679769) is the isomer of Casopitant (HY-14405). Casopitant is a NK(1)-receptor antagonist. Casopitant can be used for the research of chemotherapy-induced nausea and vomiting[1][2].
Amino-PEG2-C2-acid is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
V-11-0711 (V-11 0711) is a novel potent and selective choline kinase alpha (ChoKα) inhibitor with IC50 of 20 nM, with 11 fold less activity against ChoKβ; exhibits excellent selectivity against a panel of 50 kinases; impedes the catalytic activity and causes a reversible growth arrest, reduces phosphocholine (Pcho) in Hela cells with IC50 of <1 uM; also shows synergetic cytotoxic effects combined with chemotherapeutic temozolomide in some cancer cell lines.
Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects[1].
SCO-PEG3-COOH is a PROTAC linker and belongs to the PEG class. SCO-PEG3-COOH contains SCO and COOH that can be covalently combined with amino groups respectively. SCO is often used to react with amino acid residues of proteins or peptides, particularly lysine.
SARS 3CLpro-IN-1 (Compound 3b) is a SARS 3CL protease inhibitor with an IC50 value of 95 μM, as a specific stereo isomerof the octahydroisochromene scaffold, directs the P1 site imidazole[1].
BMS-794833 is a VEGFR2 and Met inhibitor extracted from patent WO2009094417, compound example 1; has IC50s of 15 and 1.7 nM, respectively.
Benzo[a]pyrene-d12 is the deuterium labeled Benzo[a]pyrene[1]. Benzo[a]pyrene shows lung carcinogenicity in animal models, and it is frequently used in chemoprevention studies[2][3].
VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.IC50 value: Target: 130/250/250/330/2.3/4.7 nM(Ki for cathepsin S/L/ZV/Bhumanized-rabbit cathepsin K/cathepsin F) [1]VBY-825 is a potent inhibitor of the assayed cathepsins and its potency against at least one cathepsin, cathepsin S, extends across species relevant for pharmacology studies, specifically mouse. 10 mg/kg/day dose of VBY-825 achieves a trough plasma concentration >200nM, which is well above that required for full inhibition of the intracellular activity of cathepsins B, F, K, L, S and V in both mouse and human cell lines.
CDK7-IN-25 (CY-16-1) is a CDK-7 inhibitor (IC50<1nM) that can be used in cancer research[1].
TCO-PEG6-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Soyasaponin III, a monodesmodic oleanane triterpenoid, is one of the main potentially bioactive saponins found in soy (Glycine max) and related products. Soyasaponin III can induce apoptosis in Hep-G2 cells[1].
KRAS G12C inhibitor 30 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 2. KRAS G12C inhibitor 30 can be used for the research of cancer[1].
SHP836 is a distinct, allosteric site 2 SHP2 inhibitor with IC50 of 12 uM (SHP2 1-525), and selective over the phosphatase domain (SHP2 PTP IC50>100 uM).downregulates DUSP6 mRNA, a downstream MAPK pathway marker, in KYSE-520 cancer cells; enhances pharmacological pathway inhibition in cells combined with SHP099.
Ceritinib D7 (LDK378 D7) is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor[1].
AR-A014418-d3 (AR 0133418-d3) is the deuterium labeled AR-A014418. AR-A014418 is a potent, selective, and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM)[1].
KRAS G12C inhibitor 19 is a potent inhibitor of KRAS G12C. KRAS G12C inhibitor 19 significantly inhibits tumor growth (extracted from patent WO2021118877A1)[1].
5’-O-(p-Toluoyl)-2’-O-acetyl-3’-deoxy-3’-fluoro-6-chloroinosine 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].