L-Cysteine ethyl ester HCl is a cysteine derivative[1].
SDF-1α (human) is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) can be used in cardiovascular disease research[1][2].
Ilexgenin A is a pentacyclic triterpenoid, which extracted from Ilex hainanensis Merr. Ilexgenin A can be used for the research of inflammation and cancer[1].
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2[1][2]. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity[3][4].
AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene[1].
H-His-Phe-OH is adipeptide.
2′-Deoxy-2′-fluoro-3-deaza-arabinouridine 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].
3-O-Methylquercetin (3-MQ), a main constituent of Rhamnus nakaharai, inhibits total cAMP and cGMP-phosphodiesterase (PDE) of guinea pig trachealis. 3-O-Methylquercetin (3-MQ) exhibits IC50 values of 31.9 μM， 86.9 μM， 18.6 μM and 1.6 μM for PDE1, PDE5, PDE2 and PDE4, respectively[1].
NH2-PEG9-acid is a non-cleavable 9 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
DUPA(OtBu)-OH is a DUPA precursor. DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.
8-Methylthio-adenosine is an adenosine analogue. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. The popular products in this series are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability[1].
Fmoc-His(Fmoc)-OH is a histidine derivative[1].
Cetirizine, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. IC50 value:Target: Histamine H1 receptorCetirizine crosses the blood-brain barrier only slightly, reducing the sedative side-effect common with older antihistamines. It has also been shown to inhibit eosinophil chemotaxis and LTB4 release. At a dosage of 20 mg, Boone et al. found that it inhibited the expression of VCAM-1 in patients with atopic dermatitis. The levorotary enantiomer of cetirizine, known as levocetirizine, is the more active form. From Wikipedia.
GDC-0941 dimethanesulfonate is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
9,10-Anthracenediyl-bis(methylene)dimalonic acid (ABMDMA) is a biological dye and indicator used to detect singlet oxygen generation (SOG). 9,10-Anthracenediyl-bis(methylene)dimalonic acid is water-soluble derivative of anthracene. 9,10-Anthracenediyl-bis(methylene)dimalonic acid can be photobleached by singlet oxygen to its corresponding endoperoxide. This reaction can be monitored spectrophotometrically by recording the decrease of absorbance at 400 nm[1][2].
VU0424238 is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). VU0424238 has an acceptable CNS penetration[1].
SC40230 is a class I antiarrhythmic agent.
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain[1].
7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.IC50 value: 0.86 uM(Lactate uptake inhibition) [1]Target: MCT inhibitor; lactate transport inhibitorContrary to the reference MCT1 inhibitor AR-C155858, 7ACC unexpectedly inhibited lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters. 7ACC delayed the growth of cervix SiHa tumors, colorectal HCT116 tumors, and orthoptopic MCF-7 breast tumors. MCT target engagement was confirmed by the lack of activity of 7ACC on bladder UM-UC-3 carcinoma that does not express functional MCT. 7ACC also inhibited SiHa tumor relapse after treatment with cisplatin. Finally, we found that contrary to AR-C155858, 7ACC did not prevent the cell entry of the substrate-mimetic drug 3-bromopyruvate (3BP) through MCT1, and contributed to the inhibition of tumor relapse after 3BP treatment.
RAD51-IN-17 is a quinazolinone derivative that inhibts homologous recombinase RAD51, effectively inhibits both RAD51 foci formation in response to DNA damage, and proliferation of TNBC cell lines; also sensitizes aggressive metastatic TNBC to DNA damage induced by irradiation; a valuable research tool for developing combination therapies to overcome RAD51 driven resistance and relapse in a variety of cancers.
Antazoline is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect[1][2][3].
Disulfamide, an orally active diuretic, is a carbonic anhydrase inhibitor with the IC50 value of 0.07 μM. Disulfamide leads to diuresis by inhibiting carbonic anhydrase and preventing the reabsorption of sodium and bicarbonate in the proximal tubule[1].
CDK7-IN-17 is a potent inhibitor of CDK7. CDK7-IN-17 is a pyrimidinyl derivative compound. CDK7-IN-17 has the potential for the research of various cancers, especially the cancer with transcriptional dysregulation (extracted from patent CN114249712A, compound 1)[1].
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Dihydropyrocurzerenone is a furanosesquiterpene isolated from the resin of Commiphora sphaerocarpa[1].
Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis[1].
7-O-Methyl-6-Prenylnaringenin is an active compound. 7-O-Methyl-6-Prenylnaringenin can be isolated from Humulus lupulus[1].
PK095 is a p53 mutant stabilizer. PK095 can be used for research of cancer[1].
1,3-Dinitroglycerin-d5 is the deuterium labeled 1,3-Dinitroglycerin[1].