Boc-L-Pra-OH (DCHA) is a click chemistry reagent containing an azide group. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity[1].
Valeriotetrate C, a compound isolated from Valeriana jatamansi Jones, exhibits neuroprotective activity[1].
Cavα2δ-IN-1 shows high selectivity for voltage-gated calcium channels Cavα2δ-1 (Ki 6 nM) versus Cavα2δ-2 (Ki ＞ 10000 nM).
Dilmapimod (SB-681323) is a potent p38 MAPK inhibitor that potentially suppresses inflammation in chronic obstructive pulmonary disease.
Ralpancizumab is a selective PCSK9 inhibitor with potential application in hemorrhagic stroke[1].
Novel capsid targeted inhibitor of HIV-1 replication
L-Leucine-18O2 is the 18O-labeled L-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway[1].
Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization[1][2].
Colistin (Polymyxin E) is an orally active polypeptide antibiotic and has excellent activity against various Gram-negative rod-shaped bacteria, including multidrug-resistant Pseudomonas aeruginosa, Acinetobacter baumannii and Klebsiella pneumoniae. Colistin (Polymyxin E) is associated with nephrotoxicity and can be used for the research of infections caused by Gram-negative bacilli[1][2].
YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.IC50 value:Target: BCRP inhibitorin vitro: YHO-13177 potentiated the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38–resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiated the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. In contrast, it had no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells and multidrug resistance-related protein 1–mediated doxorubicin resistance in MRP1-transfected human epidermoid cancer KB-3-1 cells. YHO-13177 increased the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppressed the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1].in vivo: In mice, YHO-13351 was rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increased the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone had little effect in these tumor models [1].
Lactulose is a non-absortable sugar used in the treatment of constipation and hepatic encephalopathy. It generally begin working after eight to twelve hours but may take up to two days to improve constipation.
CDD-1845 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 3 nM. CDD-1845 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants[1].
Talmapimod (SCIO-469) is a selective ATP-competitive p38 inhibitor with IC50 of 9 nM for p38α.
Oleaside A is a polar cardenolide monoglycoside isolated from Nerium oleander, inhibits the induction of ICAM-1 induced by IL-1α and TNF-α, and has anti-tumor activity[1].
2-Phenylethanamine hydrochloride is believed to function as a neuromodulator or neurotransmitter.
Fmoc-alpha-allyl-L-alanine is an Fmoc-protected alanine derivative.
Efmoroctocog alfa is a fully recombinant factor VIII-Fc fusion protein (rFVIIIFc) with an extended half-life compared with conventional factor VIII (FVIII) preparations, including recombinant FVIII (rFVIII) products such as Moroctocog alfa1. It is an antihemorrhagic agent used in replacement therapy for patients with haemophilia A (congenital factor VIII deficiency). It is suitable for all age groups. Haemophilia A is a rare bleeding disorder associated with a slow clotting process caused by the deficiency of factor VIII. Patients with this disorder are more susceptible to recurrent bleeding episodes and excessive bleeding following minor traumatic injuries or surgical procedures 1. Prophylactic treatment may dramatically improve the management of severe haemophilia A in the future by reducing joint bleeding and other hemorrhages that cause chronic pain and disability to patients 1,2. Prophylaxis has also shown to reduce the formation of neutralizing anti-FVIII antibodies, or inhibitors 2.Factor VIII is a blood coagulant factor involved in the intrinsic pathway to form fibrin, or a blood clot. Efmoroctocog alfa is a first commercially available rFVIII-Fc fusion protein (rFVIIIFc) where the conjugated molecule of rFVIII to polyethylene glycol is covalently fused to the dimeric Fc domain of human immunoglobulin G1, a long-lived plasma protein Label. The B domain of factor VIII is deleted. In animal models of haemophilia, efmoroctocog alfa demonstrated an approximately two-fold longer t½ than commercially available rFVIII products 1.
EG-011 is the first-in-class and potent Wiskott-Aldrich syndrome protein (WASP) activator. EG-011 activates the auto-inhibited form of WASP with strong actin polymerization. EG-011 has selective anti-tumor activity in lymphomas[1][2][3].
CGP 35348 is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM. CGP 35348 shows affinity for the GABAB receptor only[1]. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage[2].
Nek2/Hec1-IN-2 (Compound 14) is an inhibitor of Nek2/Hec1. Nek2/Hec1-IN-2 inhibits cancer cell proliferation with IC50 >25 μM[1].
Guajadial C is a Top1 catalytic inhibitor that delays Top1 poison-mediated DNA damage. Guajadial C shows cytotoxicity against cancer cells[1].
CTX-471 is a fully human monoclonal antibody of CD137. CTX-471 has bind affinity for recombinant human, cynomolgus macaque CD137 and mouse CD137 with Kd values of 50 nM, 61 nM and 748 nM, respectively. CTX-471 can be used for the research of immunomodulation and cancer[1].
Azido-PEG7-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5-Fluorouracil-13C4,15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
Ladanein is a flavonoids compound isolated from Thymus piperella[1].
Suc-AAPR-pNA is a substrate of trypsin acyl-enzymes. Suc-AAPR-pNA can be used to test trypsin acyl-enzymes activity[1][2].
Tolterodine Tartrate(PNU-200583E; Kabi-2234) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo. IC50 Value:Target: mAChRin vitro: Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors [1].in vivo: Tolterodine was extensively metabolized in vivo [2]. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased [3].
Cisd2 agonist 2 (compound 6) is an orally active Cisd2 activator (EC50=191 nM), while the Cisd2 levels is correlated with nonalcoholic fatty liver disease (NAFLD). Cisd2 agonist 2 has no significant toxicity in vivo in Cisd2hKO-het mice (heterozygous hepatocyte-specific Cisd2 knockout)[1].
AM12 inhibits Lanthanide-evoked TRPC5 activity with an IC50 of 0.28 μM[1].
Safusidenib is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma[1]. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively[2].