AAK1-IN-1(BMS-986176) is a chemical probe for AAK1 and BIKE that potently targets the ATP-binding site (AAK1 Ki = 9.1 nM; BIKE Ki = 17 nM). Regarding kinase selectivity, only three kinases were observed to bind SGC-AAK1-1 within 30-fold of the KD of AAK1 in a KINOMEscan assay (DiscoverX) at 1 μM followed by KD determinations: RIOK1 (KD = 72 nM), RIOK3 (KD = 290 nM), and PIP5K1C (KD = 260 nM). In a live cell NanoBRET assay (Promega) SGC-AAK1-1 has potency for ectopically expressed full-length AAK1- and BIKE-Nluc fusion proteins (AAK1 IC50 = 230 nM; BIKE IC50 = 1.5 μM).

ADX-102 (Reproxalap, NS-2) is a novel small molecule immunomodulator that covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal, which have been shown to mediate inflammatory pain; DX-102 is a promising agent for the treatment of dry eye disease.

OTS186935 (OTS-186935) is a potent, in vivo-active inhibitor of protein methyltransferase SUV39H2 with IC50 of 6.49 nM, inhibits A549 cell growth with IC50 of 0.67 uM; causes a significant growth inhibitory effect in mouse xenograft models using MDA-MB-231 breast cancer cells as well as A549 lung cancer cells, at 25 mg/kg once daily for 14 days yielded a TGI of 60.8%; attenuates the levels of H3K9me3 in A549 xenograft mouse model.

MDI-2268 (MDI2268) is a small-molecule, in vivo-active inhibitor of plasminogen activator inhibitor type-1 (PAI-1), demonstrates excellent pharmacokinetics, potent activity against vitronectin-bound PAI-1 in vivo, and efficacy in murine model of venous thrombosis.

SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..

UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD.

AZD-7986(Brensocatib) is a highly potent, reversible, and selective DPP1 inhibitor with enzyme and cell pIC50 of 8.4.

5-Lipoxygenases (15-LO) inhibitor 1 is a heterocyclic pyrimidobenzothiazine compound that inhibits 15-LO with an IC50 value of 18 µM.

CBS-1117 is a novel fusion inhibitor with EC50 ∼3 μM against group 1 HA.

Tafluprost(AFP-168) is an anti-glaucoma prostaglandin (PG) analog.A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.1,2,3,4 Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency.

CC-90011 is a potent and orally active LSD1 inhibitor. CC-90011 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively. CC-90011 exhibits potent on-target induction of cellular differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cell lines, and antitumor efficacy in patient-derived xenograft (PDX) SCLC models.

Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain.

Osilodrostat is an inhibitor of aldosterone synthase and aromatase, for treating Cushing’s disease.

BAY 80-6946(Copanlisib) is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM.

STING agonist 4 is an amidobenzimidazole (ABZI)-based compound that functions as a STING agonist with Kd of 1.6 nM (binding of endogenous full-length STING, THP-1 cell lysates); caused dose-dependent phosphorylation of IRF3 and STING that was inhibited by the TBK1 inhibitor BX795, induced dose-dependent secretion of IFN-β with EC50 of 3.1 uM in PBMCs (18-fold more potent than cGAMP); promotes production of IFN-γ-induced protein 10 (IP-10), IL-6 and TNFα by a mechanism that is dependent on STING-mediated activation of TBK1; unlike cGAMP and DMXAA, compound 2 efficiently activates STING function while maintaining an open STING confirmation.

Butoconazole is an imidazole antifungal used in gynecology. It is administered as a vaginal cream.

(+)-Praeruptorin A is a coumarin derivative originally isolated from P. praeruptorum.

(±)-SLV 319 is a potent and selective CB1 receptor antagonist (Ki = 7.8 nM). Exhibits 1000-fold selectivity for CB1 over CB2 receptors.

(20R)-Protopanaxdiol has protective effect on myocardial ischemia, which may be related to improving free radicals metabolism and myocardial metabolism, decreasing plasma TXA 2 levels.

(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin; apoptosis inducer.

(S)-(-)-Perillyl alcohol is a monoterpenoid compound found in the essential oils of cherries, lavender and spearmint.

(S)-Equol preferentially binds ERβ (Ki = 0.73 nM) and demonstrates approximately 9-fold lower affinity for ERα (Ki = 6.41 nM).

. For the detailed information of RGW 611, the solubility of RGW 611 in water, the solubility of RGW 611 in DMSO, the solubility of RGW 611 in PBS buffer, the animal experiment (test) of RGW 611, the cell expriment (test) of RGW 611, the in vivo, in vitro and clinical trial test of RGW 611, the EC50, IC50,and affinity,of RGW 611, Please contact DC Chemicals..

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CLP290 (CLP-290) is an orally acirtve small molecule K+-Cl- cotransporter isotype 2 (KCC2) activator, the carbamate prodrug of CLP257; In vivo co-treatment with morphine and oral CLP290 prevented membrane KCC2 downregulation in SDH neurons. Concurrently, co-treatment with CLP290 significantly mitigated MIH and acute administration of CLP257 in established MIH restored normal nociceptive behavior.

10-Desacetyl Paclitaxel is a semi-synthetic precursor of Paclitaxel that is used for biochemical research purposes.

11-keto-β-Boswellic acid is a naturally occurring pentacyclic triterpene isolated from the gum resin exudate from the stem of the tree B. serrata (frankincense).

13-Acetyl-9-dihydrobaccatin-III is an apoptosis inducer.

1400W dihydrochloride is a slow, tight binding, potent and highly selective inhibitor of inducible nitric oxide synthase (Kd = 7 nM).

1A-116 is a specific Rac1 inhibitor.