WM-1119 is a highly potent and selective KAT6A inhibitor, with an IC50 of 0.25 μM for KAT6A in lymphoma cells, the binding KD values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively.
PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. PFI-90 induces apoptosis and myogenic differentiation, resulting in the cell death increased. PFI-90 has the potential for the antitumor activity. (patent WO2021101929A1).
STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis[1].
cIAP1 Ligand-Linker Conjugates 16 is an E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs.
2-O-β-D-Glucopyranosyl-L-ascorbic acid (AA-2βG), isolated from Lycium Fruit, is a stable vitamin C analog with anti-tumor activity[1].
Pierreione B is a pyranoisoflavone, that can be isolated from the leaves and twigs of Antheroporum pierrei. Pierreione B demonstrates solid tumor selectivity with minimal cytotoxicity[1].
KDM5-C49 is a potent, selective KDM5 inhibitor with IC50 of 25, 30 and 59 nM for KDM5A, B and C, respectively; displays 25-100-fold selectivity over KDM6B, 2-30-fold selectivity over KDM4 family, but with less cell-permeablity.
Folinic acid (Leucovorin) disodium is a biological folic acid and is a forms of vitamin B9. Folinic acid disodium is generally administered along with Methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity. Folinic acid disodium and Sfluorouracil adjuvant chemotherapy shows effective in colon carcinoma[1][2][3].
Tetrandrine is a bis-benzyl-isoquinoline alkaloid, which inhibits voltage-gated Ca2+ current (ICa) and Ca2+-activated K+ current.
SB-431542 is a potent and selective inhibitor of ALK5 with an IC50 value of 94 nM, and is also an inhibitor of TGF-β Receptor.
GLPG0634 is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
3-O-α-L-Rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl hederagenin28-O-β-D-xylopyranosyl-(1→6)-β-D-glucopyranosyl ester is a hederagenin-type saponin with antitumor and anti-inflammatory properties[1].
Mal-PEG3-NH2 TFA is a linear heterobifunctional PEG crosslinker with Maleimide (HY-W007324) and amine. Mal-PEG3-NH2 TFA is a non-degradable (non-cleavable) PROTAC linker[1].
Omipalisib (GSK2126458) is a highly selective and potent inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively.
PF-07265807 (PF 07265807) is a potent, selective dual Axl/Mer inhibitor, blocks Axl- and Mer-mediated signal transduction pathways, and inhibits proliferation and migration of Axl- and Mer-overexpressing tumor cells.
SCH-1473759 is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively.
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies[1].
Monomethyl auristatin E intermediate-5 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs)[1].
Linavonkibart (SRK 181) is a high-affinity, fully human antibody that selectively binds to latent TGFβ1 and inhibits its activation. Linavonkibart plays an important role in cancer[1].
Androgen receptor degrader-2 (compound 9) is a potent androgen receptor degrader. Androgen receptor degrader-2 can be used in research of cancer[1].
Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3±0.07.
8-Methyl-2’-deoxyadenosine 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].
SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
Enpp-1-IN-8 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-8 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51)[1].
ZINC00640089 is a specific Lipocalin-2 (LCN2) inhibitor. ZINC00640089 inhibits cell proliferation, cell viability and reduces AKT phosphorylation levels in SUM149 cells. ZINC00640089 has good potential for research in inflammatory breast cancer (IBC)[1].
Neohelmanthicin A (compound 3A) is a phenylpropanoid compound with antitumor activity. The IC50s of Neohelmanthicin A for inhibiting leukemia cell line EL4, breast cancer cell line S180 and breast cancer cell line MCF7 are 0.13 μM, 7 μM and 23 μM respectively[1].
Cbz-Phe-(Alloc)Lys-PAB-PNP is an cleavable linker for antibody-drug conjugates (ADC) design.
Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer[1][2].
E3 ligase Ligand 19 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 19 can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4[1]。
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.