FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia[1].
MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system[1]. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo[2].
TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors[1].
Trichorabdal A is a diterpenoid compound isolated from Rabdosia trichocarpa. Trichorabdal A has potent anti-tumor activity[1].
Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines[1][2].
LSD1-UM-109 is a ighly potent and reversible LSD1 inhibitor with an IC50 of 3.1 nM. LSD1-UM-109 inhibits cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line[1].
Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
Tetrahydrouridine is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
Bromo-PEG3-C2-phosphonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB)[1][2].
(+)-Usnic acid is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usnic acid inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity[1].
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice[1][2].
Ipomoeassin F is a potent and selective endoplasmic reticulum (ER) protein-translocation inhibitor by targeting the pore-forming subunit of the Sec61 complex (Sec61α) at the ER membrane. Ipomoeassin F selectively inhibits the ER membrane translocation of SARS-CoV-2 proteins. Ipomoeassin F block the ER translocation of secretory proteins and type I transmembrane proteins (TMPs), but not type III TMPs[1][2][3].
N-tert-Butoxycarbonyl-trans-4-hydroxy-D-proline is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-tert-Butoxycarbonyl-trans-4-hydroxy-D-proline is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
Thalidomide-5-O-C2-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].
PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM)[1].
(R)-Edelfosine ((R)-ET-18-OCH3) is a ether lipid analog with anti-HIV and antineoplastic activity[1].
BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.
Licochalcone D, a flavonoid compound mainly existing in the root of Glycyrrhiza inflate, is a potent inhibitor of NF-kappaB (NF-κB) p65. Licochalcone D possesses antioxidant, anti-inflammatory, anti-cancer properties[1][2].
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM[1].
CHIR-99021 monohydrochloride is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
diMal-O-CH2COOH is a cleavable ADC linker.
Choline-13C2 (chloride) is the 13C labeled Choline chloride[1]. Choline chloride is an essential nutrient that activates alpha7 nicotinic receptors and has analgesic and anti-inflammatory activity. Glycerophosphoinositol choline can affect diseases such as liver disease, atherosclerosis and neurological disorders[2][3].
PROTAC Linker 9 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 9 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].
CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. CBP501 Affinity Peptide can be used in cancer research[1].
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer[1].
5,8,11-Eicosatriynoic acid (ETI) is a lipoxygenase inhibitor that blocks LTC4 biosynthesis in mast cell tumor cells[1].
CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively[1][2].
Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with Kis of 3.0, 4.4 and 3.4 nM, respectively.