20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells[1][2].
gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's diseaseIC50 value: Target: γ-secretaseγ-secretase modulator is modulation of the action of γ-secretase so as to Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain. γ-secretase modulator is usful in particular Alzheimer's disease.
LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (Kds<2 nM). HSD1590 displays low cytotoxicity[1].
ARN25068 is a sub-micromolar inhibitor of the three protein kinases, GSK-3β, FYN and DYRK1A to tackle tau hyperphosphorylation[1].
Tyk2-IN-8 (Compound 3) is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. Tyk2-IN-8 inhibits JAK1-JH1 with IC50 of 3.0 nM. Tyk2-IN-8 can be used for the research of autoimmune disease[1].
Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway. Hedgehog IN-5 can be used for the research of fibrotic disease[1].
GSK-3β inhibitor 9 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. GSK-3β inhibitor 9 shows good pharmacokinetic profiles including favorable BBB penetration. GSK-3β inhibitor 9 can be used for the research of Alzheimer’s disease[1].
FLI-06 is an inhibitor of Notch signaling with an EC50 of 2.3 μM.
GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM[1][1][2].
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable drug metabolism and pharmacokinetics profile[1].
N-Salicyloyltryptamine acts on voltage-dependent Na+, Ca2+, and K+ ion channels inhibitor. N-Salicyloyltryptamine inhibits K+ currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect[1]-[5].
CCT 365623 (CCT365623) hydrochloride is a potent, orally active small molecule inhibitor of lysyl oxidase (LOX) with IC50 of 0.89 uM; inhibits LOX actvity in living cell system (MDCK cysts) at 5 uM, reduces EGFR retention at the cell surface, suppresses EGFR and AKT phosphorylation driven by EGF, also activates SMAD2 and downregulates MATN2; delays the growth of primary and metastatic tumour cells in vivo.
Chrysomycin A (Chr-A), an antibiotic, can be obtained from Streptomyces. Chrysomycin A exhibits antitumor and anti-tuberculous and MRSA activities. As for glioblastoma, Chrysomycin A inhibits the proliferation, migration, and invasion of cancer cells through the Akt/GSK-3β/β-catenin signaling pathway[1].
JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM)[1].
Robotnikinin is a small molecule capable of binding to and inhibiting the activity of Sonic Hedgehog (Shh) signaling up stream of Smo[1][2].
(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer[1].
Momelotinib-d2 (CYT387-d2) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally active and ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively, shows much less activity against JAK3[1][2].
JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
Crenigacestat (LY3039478) is a novel and potent Notch inhibitor.
ERK2 IN-1 is a selective ERK2 inhibitor with an IC50 of 7 nM[1].
H-1152 is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
Carvacrol is a monoterpenoid phenol isolated from Lamiaceae family plants, with antioxidant, anti-inflammatory and anticancer properties. Carvacrol causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis[1].
ERK-IN-3 is a potent and oral inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.[1].
Fasudil Hydrochloride is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Kis of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.
Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
Balsalazide-d4 is deuterium labeled Balsalazide. Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases[1]. FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.