Furamidine-d8 (DB75-d8) is the deuterium labeled Furamidine. Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent[1][2][3].
Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
A18-Iso5-2DC18 (compound A18) is a cyclic lipidoid that can facilitate mRNA protein expression and induce a strong immune response mediated[1].
L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 inhibits LPS-induced inflammation, particularly TNF-α and IL-6 production and gene expression in mouse macrophages. L48H37 is used for the research of sepsis or lung injury treatment[1].
AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice. AR-C118925XX also inhibits ATP-induced tumor growth[1][2].
CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB[1]. CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats[2].
CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC50s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders[1].
PAD2-IN-1, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-1 shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold)[1].
nti-inflammatory agent 49 (compound SC9) is a quite potent and selective inhibitor of Drp1-Fis1 interaction and can reduce FIS1-mediated mitochondrial dysfunction. The IC50 of SC9 inhibiting GTPase in vitro is 270 nM[1].
L-Lysine-13C dihydrochloride is the 13C-labeled L-Lysine dihydrochloride. L-lysine dihydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.
PF-06651600 is a potent JAK3-selective inhibitor with an IC50 of 33.1 nM.
PD1-IN-2 is a PD1 signaling pathway inhibitor, which acts as an immunomodulator.
TP-030-1 is an inhibitor of RIPK1. TP-030-1 inhibits hRIPK1 with a Ki value of 3.9 nM and inhibits mRIPK1 with an IC50 value of 4.2 μM. TP-030-1 can be used for the research of inflammatory diseases and neurodegenerative diseases[1].
RGX-104 (free base) is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
BTK-030 is a novel BTK inhibitor.
Glycosmisic acid, a natural compound, possesses anti-HBV activity[1].
Pasakbumin B, a bioactive compound from Eurycoma longifolia Jack, exhibits potent antiulcer activity[1].
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties[1][2][3][4].
Loureirin C, isolated from "Dragon’s blood", which is a deep red resin obtained from a variety of plant sources. The resin extracted from stems of Dracaena cochinchinensis is one such source of “dragon’s blood”, has a reputation for facilitating blood circulation and dispersing blood stasis. The resin has anti-bacterial, anti-spasmodic, anti-inflammatory, analgesic, anti-diabetic, and anti-tumor activities[1].
Coronalolic acid, extract from the apical bud of Gardenia sootepenesis Hutch, inhibits TNF-α-induced NF-κB activity and NO production[1].
Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid potassium can directly trigger cancer cells to undergoApoptosis[1][2][3].
Azido-PEG4-C2-acid a PEG-based PROTAC linker can be used in the synthesis of vRucaparib-TP4. Azido-PEG4-C2-acid is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Myricetin 3-O-α-L-arabinopyranoside is a quercetin derivative and plant flavonoid with antioxidant, antibacterial and antiurease effects. Myricetin 3-O-α-L-arabinopyranoside inhibits A2E photooxidation-induced RPE cell death. Myricetin 3-O-α-L-arabinopyranoside is protective against retinal degeneration and protects against blue light (BL)-induced damage in RPE cells and mouse models[1].
3,4,5-Tricaffeoylquinic acid is isolated from barks of Ilex rotunda Thunb, used in the research of the pro-inflammatory mediator-induced skin disease[1].
SEMBL is a potent NF-κB inhibitor that inhibits DNA binding of NF-κB component p65; inhibits LPS-induced NF-κB activation, iNOS expression, and inflammatory cytokine secretions; also inhibits NF-κB and cellular invasion in ovarian carcinoma ES-2 cells; enhances stability in aqueous solution compared with (-)-DHMEQ.
Protirelin is a highly conserved neuropeptide that exerts the hormonal control of thyroid-stimulating hormone (TSH) levels as well as neuromodulatory functions.
GNE-4997 is a potent and selective ITK/TSK inhibitor.
RIPK1-IN-16 is an orally active and potent inhibitor of RIPK1. RIPK1-IN-16 inhibits excessive inflammation by blocking RIPK1-mediated necroptosis in vivo. RIPK1-IN-16 protects mouse from TNF-induced systemic inflammatory response syndrome and sepsis[1].
Raddeanoside R17 (Pulchinenoside E3) is a saponins compound that can be isolated from the root of Pulsatilla koreana. Raddeanoside R17 shows anti-inflammatory effects[1][2].
ROCK-IN-32 is an effective Rho-kinase inhibitor.