Ontorpacept (TTI-621) is a soluble fusion protein that consists of the human SIRPα N-terminal (1-118) linked to the Fc region of human IgG1. The N-terminal (1-118)-fragment of ontorpacept is a binding domain for CD47 which is an inhibitor of phagocytosis by macrophages. Ontorpacept is a CD47-blocking checkpoint inhibitor with antitumor activity[1].
w-Conotoxin SVIB is a peptide toxin, it can be isolated from Conus venoms. w-Conotoxin SVIB inhibits twitch response with an IC50 value of 37 nM. w-Conotoxin SVIB induces respiratory distress and it can be lethal to mice at a high concentration[1][2].
(-)-Gallocatechin, an epimer of (-)-Epigallocatechin (EGC), is contained in various tea products. (-)-Gallocatechin has antioxidant activities[1][2][3].
2-Methyl-1,3,6-trihydroxy-9,10-anthraquinone 3-O-α-rhamnosyl-(1→2)-β-glucoside is anthraquinone glycoside found in the dried roots of Rubia cordifolia[1].
Undecylprodigiosin is a cytotoxic immunosuppressant[1].
Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3. Lepzacitinib exhibits anti-inflammatory effect and inhibits atopic dermatitis and other skin diseases[1].
CRBN-6-5-5-VHL is a potent and selective cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3[1].
Lithocholic acid-d5 is deuterium labeled Lithocholic acid.
9-(2’-O-Acetyl-5’-O-benzoyl-3’-O-methyl-beta-D-ribofuranosyl)-6-chloropurine 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].
PF-06447475 trihydrochloride is a highly potent, selective, brain penetrant LRRK2 kinase inhibitor with IC50 values of 3 nM and 11 nM for WT LRRK and G2019S LRRK2, respectively. PF-06447475 trihydrochloride can be used for parkinson's disease (PD) research[1].
Tafluprost ethyl amide is a prostaglandin derivative. Tafluprost ethyl amide is capable of intraocular pressure (IOP) reduction and influencing eyelash growth. Tafluprost ethyl amide can be used in antiglaucoma ophthalmic compositions or cosmetics[1].
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM[1].
Fmoc-Asn-OH is an asparagine derivative[1].
IBS008738 is a potent TAZ activator. IBS008738 stabilizes TAZ, increases the unphosphorylated TAZ level, enhances the association of MyoD with the myogenin promoter, upregulates MyoD-dependent gene transcription, and competes with myostatin in C2C12 cells. IBS008738 enhances myogenesis in C2C12 cells and facilitates muscle repair in a muscle injury model[1][2].
2-Amino-2-(4-hydroxyphenyl)acetic acid is a Glycine (HY-Y0966) derivative[1].
Nystatin A3, produced by Streptomyces noursei, a biologically active component of nystatin complex. Antibiotic activity[1]
PRMT5-IN-3 is a PRMT5 inhibitor that exhibits synthetic lethality to tumor cells but produce few side effects combined with DNA damaging agents.
Curcolonol is a furan type sesquiterpene. Curcolonol can be isolated from several medical herbs. Curcolonol has inhibitory activity for LIM kinase 1. Curcolonol can be used for the research of breast cancer[1].
DTSSP Crosslinker is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Fmoc-D-Dbu(N3)-OH is a click chemistry reagent containing an Azide[1].
Head activator neuropeptide is a mitogen for mammalian cell lines of neuronal or neuroendocrine origin. Head activator neuropeptide signals by binding GPR37 and stimulates cells to enter mitosis[1].
1,5,5-Trimethylhydantoin (TMH) is a non-isotopic internal standard (IS)[1].
PYZD-4409 is a novel small molecule inhibitor of Ubiquitin-activating enzyme UBA1/E1 enzyme with an IC50 of 20 uM (cell-free enzymatic assay).IC50 Value: 20 uM (cell-free enzymatic assay) [1]Target: E1 enzyme (Ubiquitin-activating enzyme)in vitro: PYZD-4409 inhibited the ATP-dependent activation of ubiquitin and subsequent transfer of the activated ubiquitin from the E1 to the common human E2 enzyme UBE2E2 in a gel-based assay. The IC50 of inhibition was estimated to be 20μM in a cell-free enzymatic assay. Suggesting specificity of PYZD-4409 for the E1 enzyme, the compound had no effect on unrelated enzymes such as α-Mannosidase II glycosylation enzyme or Luciferase at concentrations up to 100μM (data not shown). It also did not inhibit the summo E1, Uba2, at concentrations up to 100μM. In 5 of 8 leukemia and myeloma cell lines, PYZD-4409 induced cell death with a LD50 less than 10μM. Myeloma cell lines were particularly sensitive to E1 inhibition because PYZD-4409 induced cell death with 3 of 4 myeloma cell lines (ie, LP1, KMS11, and U226) having an LD50 of 3μM or less. In contrast, solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20μM [1]. in vivo: SCID mice were injected subcutaneously with MDAY-D2 murine leukemia cells and then treated with PYZD-4409 (10 mg/kg) or buffer control intraperitoneally daily on alternate days over 8 days. Sixteen days after tumor implantation, the mice were killed, and the tumors excised and weighed. Compared with control-treated mice, treatment with PYZD-4409 delayed tumor growth and decreased tumor weight without untoward toxicity. Inhibition of the E1 can achieve an antitumor effect in vivo [1].
3-Amino-1,2,4-triazine is an inhibitor of NO synthase, and also inhibits nitrite secretion[1].
Dihydroactinidiolide, existing in plant leaves and fruits, is a potent plant growth inhibitor, a regulator of gene expression and is responsible for photo acclimation in Arabidopsis. Dihydroactinidiolide has antioxidant activity, antibacterial activity, anticancer activity and neuroprotective effect[1].
ER-Tracker Blue-White DPX is a photostable probe used to selectively label the endoplasmic reticulum for fluorescence microscopy imaging[1].
WWL123, a carbamate-based compound, is a potent and selective ABHD6 inhibitor. WWL123 can be used for research of inflammation, metabolic disorders (obesity and type II diabetes mellitus) and epilepsy[1].
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM[1].
Sulfobromophthalein (Bromosulfophthalein) disodium salt is an organic anion dye used in the study of a variety of membrane carriers expressed in animal tissues and involved in transport of drugs and metabolites[1].