M-525 is a first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction with binding IC50 of 3.3 nM in FP assays; inhibits MV4;11 (MLL fusion) and HL60 (No MLL fusion) cell growth with IC50 of 2.7 and 2,000 nM, respectively; significantly down-regulates the expression of MEIS1, HOXA9 and HOXA11 genes in a dosedependent anner at ow nanomolar concentrations, also effectively suppresses the expression of MEIS1 and HOX genes in the MOLM-13 cell line at 3 nM.
Rhamnose-13C monohydrate is the 13C labeled Rhamnose monohydrate. Rhamnose monohydrate (L-Rhamnose monohydrate) is a monosaccharide found in plants and bacteria. Rhamnose monohydrate-conjugated immunogens is used in immunotherapies. Rhamnose monohydrate c
Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 s of 13 and 38 nM, respectively.
BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A[1].
Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ−glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties[1][2].
BGB-283 is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
Biotin-PEG11-amine is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PROTAC Linker 12 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 12 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
KRAS G12C inhibitor 38 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 38 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129820A1, compound 171)[1].
Corylin is a major bioactive compound isolated from Psoralea corylifolia L; antibiotic or anticancer compound.IC50 value:Target: in vitro: Corylin showed an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 value of 1.37 uM [1].
NH2-PEG8-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IDO-IN-15 is an IDO1 inhibitor (IC50 < 0.51 nM).
Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.
HC-067047 is a potent and selective TRPV4 antagonist with IC50s of 48 nM, 133 nM, and 17 nM for human, rat, and mouse TRPV4.
Mal-VC-PAB-PNP-CDN-A is a drug-linker conjugate for ADC[1][2].
Propargyl-PEG7-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
c-ABL-IN-4 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-4 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 54)[1].
3-Methyladenine-d3 is the deuterium labeled 3-Methyladenine[1]. 3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K[2].
FD2056 is a potent and orally active PI3K inhibitor. FD2056 inhibits PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ with IC50s of 0.30, 0.80, 1.10, 0.42 nM. FD2056 also inhibits CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 of 115.95 and 2782.15 nM. FD2056 inhibits breast cancer cell proliferation with IC50s of 1.06, 0.04, 1.40 μM for MDA-MB-231, MDA-MB-468, MCF-7 cells. FD2056 also induces cancer apoptosis and inhibits tumor growth[1].
Flavokawain B (Flavokavain B) is a chalcone isolated from the root extracts of kava-kava plant and a potent apoptosis inducer for inhibiting the growth of various cancer cell lines. Flavokawain B (Flavokavain B) shows strong antiangiogenic activity. Flavokawain B (Flavokavain B) inhibits human brain endothelial cell (HUVEC) migration and tube formation with very low and non-toxic concentrations[1][2].
m-PEG4-Ms is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
FT709 is a potent and selective USP9X inhibitor, an IC50 of 82 nM. USP9X has been linked with centrosome function, chromosome alignment during mitosis, EGF receptor degradation, chemo-sensitization, and circadian rhythms[1].
IGUANA-1 is a potent inhibitor of ALDH1B1, which is a mitochondrial enzyme that promotes colorectal and pancreatic cancer. IGUANA-1 has significant inhibition against cancer cells[1].
Benzyl-PEG2-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
K03861 is a type II CDK2 inhibitor with Kd of 8.2 nM.K03861 inhibits CDK2 activity by competing with binding of activating cyclins.
DB04760 (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM[1]. DB04760 significantly reduces paclitaxel neurotoxicity and has anticancer activity[2].
Androgen receptor degrader-3 is an androgen receptor degrader. Androgen receptor degrader-3 blocks the process of androgen receptor transduction and also degrades the receptor itself. Androgen receptor degrader-3 can be used for prostate cancer research[1].
Antennapedia Peptide is a 16 amino acid peptide, originally derived from the 60 amino acid long homeodomain of the Drosophila transcription factor Antennapedia and is a member of the family of Cell-penetrating peptides.
Propargyl-PEG-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5-ALA benzyl ester hydrochloride (Benzyl-ALA hydrochloride) is a protoporphyrin precursor used as a photodetection agent. 5-ALA benzyl ester hydrochloride induces protoporphyrin IX (PPIX) accumulation in colon carcinoma cell lines[1][2].