RCM-1 is a FOXM1 inhibitor.
DB2115 (tertahydrochloride) is a potent inhibitor of myeloid master regulator PU.1. DB2115 (tertahydrochloride) has the potential for the treatment of cancers, including hematologic cancers such as leukemia, as well as other conditions associated with PU. 1 dysfunction (extracted from patent WO2017223260A1, compound DB2115) [1].
Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect[1][2][3][4].
S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes[1][2].
DNA Gyrase-IN-7 (compound 6d) is a novel Microbial DNA-Gyrase inhibitor[1].
5-Ethyluridine is a purine nucleoside analogue. 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].
Aviculin, a lignan glycoside, is a potent anticancer agent. Aviculin reduces metabolic activity on MCF-7 cells below 50%, with an IC50 of 75.47 μM. Aviculin induces breast cancer cell apoptosis through the intrinsic apoptosis pathway. Aviculin increases expression of initiator caspase-9, executioner caspase-7, and poly (ADP-ribose) polymerase (PARP). Aviculin shows an increase in the Bax/Bcl-2 ratio[1].
NO2-SPP-sulfo is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
CCG-222740 is a potent and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor[1]. CCG-222740 also is a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis[2].
L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1][2].
BTB01303 is a (glutamate release) inhibitor. Cancer cells release high levels of (glutamate), which disrupts normal bone turnover and may lead to cancer-induced bone pain. BTB01303 has the potential to improve cancer-induced bone pain[1].
4-Methylumbelliferyl octanoate is a octoate. 4-Methylumbelliferyl octanoate can be used as a s ubstrate of hog pancreatic lipase[1].
2’-Deoxy-N2,N2-dimethylguanosine 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].
M3 receptor antagonist 1 is a muscarinic M3-receptor antagonist extracted from patent WO 2008012290 A2, formula Ic.
RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.
I-287 is a potent, selective, orally active inhibitor of PAR2, negative PAR2 allosteric modulator, inhibits PAR2-mediated activation of Gq and G12/13 but not Gi/o proteins (IC50=45-390 nM);I-287 is a negative allosteric modulator (NAM) and not an orthosteric competitive antagonist of hPAR2.I-287 inhibits PAR2-mediated activation of DAG/Ca2+/PKC and RhoA/SRF-RE, as well as FAK and ERK1/2 signaling pathways, shows no effect on PAR2-mediated recruitment of βarrestin2 and receptor internalization.I-287 inhibits PAR2-induced secretion of IL-8 cytokine in vitro and reduces Freund's adjuvant (CFA)-induced paw edema model in mice.
H-Lys(Fmoc)-OH is a lysine derivative[1].
Cucurbit[8]uril is a potent, low toxicity and orally active supramolecular inducer of protein heterodimerization. Cucurbit[8]uril induces heterodimerization of methylviologen and naphthalene functionalized proteins. Cucurbit[8]uril can induce energy transfer [1][2].
Rovelizumab is a humanized monoclonal leukointegrin antibody. Rovelizumab is a monoclonal antibody directed against the CD11/CD18 cell adhesion proteins. Rovelizumab can be used for research of multiple sclerosis (MS), hemorrhagic shock, myocardial infarction (MI) and stroke[1].
hCAII-IN-1 (compound 7f) is a potent and selective inhibitor of carbonic anhydrase (CA II/IX) with Kis of 1.2 and 113.6 nM, respectively. hCAII-IN-1 has the potential for the research of cancer diseases[1].
PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16 nM, displays >2000-fold functional selectivity for the human EP2 receptor over antagonist activity against the human EP1, EP3, EP4, DP1 and CRTH2 receptors.IC50 value: 16 nMTarget: EP2in vitro: PF-04418948 inhibits prostaglandin E2 (PGE2)-induced increase in cAMP in cells expressing EP2 receptors with a functional KB value of 1.8 nM. In human myometrium, PF-04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractions induced by electrical field stimulation with an apparent KB of 5.4 nM. [1]in vivo: In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of the PGE2-induced relaxation curve with a KB of 2.5 nM and an apparent KB of 1.3 nM respectively. Reversal of the PGE2-induced relaxation in the mouse trachea by PF-04418948 produced an IC50 value of 2.7 nM. Given orally, PF-04418948 attenuated the butaprost-induced cutaneous blood flow response in rats. [1] PF-04418948 competitively inhibits relaxations of murine and guinea pig trachea induced by ONO-AE1-259 and PGE2 respectively.[2]
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders[1].
Endotoxin inhibitor a synthetic peptide that binds lipid A with high affinity, thereby detoxifying LPS (HY-D1056) and preventing LPS-induced cytokine release in vivo. Endotoxin inhibitor inhibits the febrile response to LPS with very low toxicity and lethality[1].
2-(4-Methylbenzyl)thioadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Butofilolol is a potent β-blocking agent used in the research of hypertension[1].
3,7-DMF is an orally active inhibitor of TGF-β1-induced activation of HSCs. 3,7-DMF induces antioxidant genes and quenches ROS away, which can be used to study liver fibrosis[1].
L-Talose-13C-1 is the 13C labeled L-Talose[1].
Callophycin A, red seaweed derived metabolite, is potently against C. albicans. Callophycin A exhibits potent activity against drug resistance vaginal candidiasis[1].
Tulinercept (OPRX-106) is a monoclonal antibody. Tulinercept can be used for various biochemical studies[1].
Halobetasol (Ulobetasol) is a corticosteroid. Halobetasol can be used for research of severe localized psoriasis[1].