a-30

DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.

A-304121 is a histamine H(3) receptor.

TYRA-300 is an oral and selective FGFR3 inhibitor with an IC50 value of 11 nM and 25-fold, 14-fold, and 36-fold selectivity for FGFR1, FGFR2, and FGFR4, respectively, in the Ba F3 cell line for the treatment of metastatic uroepithelial carcinomas (mUCs) and chondrodysplasia.

LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8 0.8 5.3 16.7 nM for ALK1 2 3 6).

Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.

XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM).

dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, binding to MCL1 with a KD of 30 nM and activating the apoptosis mechanism by degrading MCL1.

AP-18 is a potent and selective TRPA1 inhibitor. AP-18 inhibits activation of TRPA1 induced by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 could reverse complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 could attenuate Yo-Pro uptake induced by 30 μM AITC in a concentration-dependent manner (IC50= 10.3 μM).

BRD 9757 (N-Hydroxy-1-cyclopentene-1-carboxamide) is a selective inhibitor of HDAC6 (IC50 = 30 nM).

CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.

L-161240 is an antimicrobial agent associated with lipid A biosynthesis with an IC50 value of 30 nM as determined by DEACET and a MIC value of 1-3 μg mL against wild-type E. coli.

USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy[1]. [1]. Arthur F Kluge, et al. Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2655-2659.

BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK PTK6), displaying an IC50 of 30 nM, and effectively suppresses p-SAM68 with an IC50 of 52 nM. This compound serves as a valuable tool for evaluating BRK inhibitors' efficacy in xenograft breast tumor models, enabling in vivo activity assessment.

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1 2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

BDCRB inhibits herpesvirus DNA maturation. BDCRB causes the HCMV terminase to skip the normal cleavage site and to continue to package DNA until a second cleavage site is encountered 30 kb further along the concatemer.

STING agonist-30 is a potent activator of STING-dependent immune responses, demonstrating broad-spectrum antiviral effects against viruses such as HSV (Herpes Simplex Virus), rotavirus, and SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2).

2H-Imidazo[4,5-b]pyrazin-2-one, 1,3-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-1-[(tetrahydro-2H-pyran-4-yl)methyl]- is a potent mTOR inhibitor with IC50 of 0.176 μM and >30 μM for mTOR and PI3Kα, respectively.

GRL-0496 is a potent inhibitor with an enzyme inhibitory activity against SARS-CoV 3CLpro with an IC50 of 30 nM and antiviral potency with an EC50 value of 6.9 μM.

Acetazolamide (Diamox) is a Carbonic Anhydrase Inhibitor. The mechanism of action of acetazolamide is as a Carbonic Anhydrase Inhibitor. The chemical classification of acetazolamide is Sulfonamides.

4-Nonylphenol polyethoxylate (Nonoxinol-9) is a typical surfactant used as a vaginal spermicide. Spermicides are locally acting non-hormonal contraceptives. When present in the vagina during intercourse, they immobilize inactivate damage and or kill sperms without eliciting systemic effects. 4-Nonylphenol polyethoxylate has been in use for more than 30 years as an over-the-counter (OTC) drug in creams, gels, foams and condom lubricants. It is the most commonly used spermicidal contraceptive in the UK and the USA. In several European countries, spermicides are no longer on the market.

Benzocaine is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.

Fenofibrate (Lipanthyl) is a PPARα agonist (EC50=30 μM) and is selective. Fenofibrate also inhibits cytochrome P450 isoforms, such as CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4. Fenofibrate exhibits antihyperlipidemic activity.

Terbinafine hydrochloride (KWD 2019) is a synthetic allylamine derivative structurally related to naftifine. Terbinafine is active against dermatophytes.

Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.