G280-9 is a 9 amino acid native epitope peptide. G280-9 is a relevant target expressed on melanoma.
Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research[1].
FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC50 value of 0.003 µM. FLT3-IN-18 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML)[1].
Protein degrader 1 TFA is a small molecule ligand for VHL, an E3 ligase which has been targeted in numerous PROTACs.
Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM.
TL13-12 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of TAE684 and the cereblon ligand pomalidomide; also promotes the degradation of additional kinases including PTK2 (FAK), Aurora A, FER, and RPS6KA1 (RSK1).
EZH2-IN-17 (compound 28) is a potent and orally active EZH2 inhibitor with an IC50 value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively)[1].
Tegafur-Uracil is an orally active fluoropyrimidines anticancer agent. Tegafur-Uracil inhibits thymidylate synthase. Tegafur-Uracil can be used for researching anti solid tumors[1].
CCT128930 is a potent and selective inhibitor of Akt2 (IC50 6 nM) with 28-fold selectivity over the closely related PKA kinase (IC50 168 nM), as well as 20-fold selectivity over p70S6K (IC50 120 nM).
3-Aminobenzamide is a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.
Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC50 = 0.2-0.7 nM).
TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
Boc-NH-PEG4-CH2CH2NH2 a cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
DABCYL-TNF-α-EDANS (-4 to +6) (human) is a FRET peptide substrate of tumor necrosis factor convertase (TACE)[1].
Erlotinib hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM.
Adenine is a purine derivative and a nucleobase with a variety of roles in biochemistry. Target: Nucleoside antimetabolite/analogAdenine is a nucleobase 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), andprotein synthesis, as a chemical component of DNA and RNA. The shape of adenine is complementary to either thymine in DNA or uracil in RNA.In older literature, adenine was sometimes called Vitamin B4. It is no longer considered a true vitamin or part of the Vitamin B complex. However, two B vitamins, niacin and riboflavin, bind with adenine to form the essential cofactors nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD), respectively. Hermann Emil Fischer was one of the early scientists to study adenine. Experiments performed in 1961 by Joan Oró have shown that a large quantity of adenine can be synthesized from the polymerization of ammonia with fivehydrogen cyanide (HCN) molecules in aqueous solution, whether this has implications for the origin of life on Earth is under debate.
4-Formylcolchicine is a potent anticancer agent. 4-Formylcolchicine shows cytotoxicity activity with IC50 values of 1.007, 0.128, 0.054 µM for A549, HT-29, HCT116 cells, respectively[1].
Labetuzumab govitecan (IMMU 130) is an Anti-CEACAM5/SN-38 antibody-drug conjugate (ADC). Labetuzumab govitecan consists of the antibody Labetuzumab, SN-38, and a pH-sensitive Linker. Labetuzumab govitecan can be used for research of cancers, such as colorectal cancer[1][2][3].
PI3K-IN-36 (compound A36) is a potent PI3K inhibitor. PI3K-IN-36 can be used in research of follicular lymphoma (FL)[1].
Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt[1]. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively[2].
2-Hydroxyxanthone (Compound 3) is an isoprene flavone derived from Calophyllum inophyllum. 2-Hydroxyxanthone has an obvious killing effect on K562 cells [1].
(E)-Mcl-1 inhibitor 7 (Example 34) is a Mcl-1 inhibitor (Ki: <1 nM, IC50: <500 nM). (E)-Mcl-1 inhibitor 7 can be used for research of cancers[1].
Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential treatment in cancer.
BML-280 (VU0285655-1) is a potent and selective phospholipase D2 (PLD2) inhibitor. BML-280 has the ability to prevent caspase-3 cleavage and reduction in cell viability induced by high glucose. BML-280 can be used for rheumatoid arthritis research[1][2].
Indole-3-carbinol suppresses NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist.
Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.
5’-Azido-5’-deoxy-2’-O-methyl-5-methyluridine 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].