DC7358APY29
APY29 is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation with IC50 of 280 nM and activates IRE1α RNase activity.
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Small Molecule Research Tools
2816 products · Page 11 of 59
Browse 372 research categories
DC7358DC20275LMP-744 hydrochloride
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase (Top1) inhibitor with antitumor activity[1].
View activity & pricesDC5089Ixazomib Citrate (MLN-9708)
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
View activity & pricesDC8316SBI-0206965
SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2
View activity & pricesDC3114Avagacestat (BMS-708163)
BMS-708163 is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; BMS-708163 also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition…
View activity & pricesDC1030Regorafenib (BAY73-4506,Fluoro-Sorafenib)
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
View activity & pricesDC8085Fexaramine
Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds. IC50 value:Target:in vitro: In vitro treatment of CDCA or fexaramine elevated the SHP…
View activity & pricesDC10073Dasotraline Hydrochloride
Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
View activity & pricesDC7376BMS777607
BMS 777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with…
View activity & pricesDC7705HTH-01-015
HTH-01-015 is a selective NUAK1 inhibitor (IC50 is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).
View activity & pricesDC10374TM5441
TM5441 is a plasminogen activator inhibitor-1 (PAI-1); inhibits several tumor cell lines with IC50 values between 9.7 and 60.3 μM.
View activity & pricesDC7857GSK-LSD1
GSK-LSD1 is a potent and selective inhibitor of lysine specific demethylase 1 (LSD1).
View activity & pricesDC8229Vorapaxar Sulfate (SCH 530348)
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits…
View activity & pricesDC8928Minocycline hydrochloride
Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.
View activity & pricesDC7947Ledipasvir
Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively.
View activity & pricesDC2097SB202190
SB 202190 is a cell-permeable p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38 and p38β2, respectively.
View activity & pricesDC8222G007-LK
G007-LK is a potent and selective inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively.
View activity & pricesDC8226RI-2
RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
View activity & pricesDC7853GSK2801
GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains.GSK2801 binds to BAZ2 bromodomains with dissociation constants (KD) of 136 and…
View activity & pricesDC8092L-755,507
L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM.
View activity & pricesDCAPI1568Saxagliptin Hydrochloride
Saxagliptin (rINN) is an orally active hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs.
View activity & pricesDC9283Q-VD-Oph
Q-VD-OPha is a irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPha is able…
View activity & pricesDC2050WIN-55212-2 mesylate
WIN 55,212-2 Mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.
View activity & pricesStructure information available on request
DC9910CYCLOPAMINE
Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay.
View activity & pricesDC8044GSK503
GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
View activity & pricesDC4221Teriflunomide(A-771726)
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
View activity & pricesDC8277E-2012
E 2012 is a potent γ-secretase modulator. In the present study, 9 dogs were treated with a single dose of the γ-secretase modulator E2012, the γ-secretase inhibitor LY450139, or vehicle with a dosing interval of 1…
View activity & pricesDC10173Firsocostat(ND-630,GS-0976)
Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.
View activity & pricesDC12161TAS6417
TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
View activity & pricesDC7140GSK1070916
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
View activity & pricesDC8344LY3009120
LY3009120 is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively.
View activity & pricesDC10109Q203
Q203 (IAP6) is a midazopyridine amide compound. Q203 is active against Mycobacterium tuberculosis H37Rv with an MIC50 of 2.7 nM in culture broth medium.
View activity & pricesDC10152Miquelianin (Quercetin 3-O-glucuronide)
Miquelianin (Quercetin 3-O-glucuronide) is a metabolite of quercetin and a type of natural flavonoid.
View activity & pricesDC7286A83-01
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM, respectively.
View activity & pricesDC1070MK-1775(AZD-1775,Adavosertib)
Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC50 of 5.2 nM.
View activity & pricesDC8766GSK1324726A (I-BET726)
GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
View activity & pricesDC11017ZLDI-8
ZLDI-8 (IAC-8) is a novel Notch signaling pathway inhibitor for Notch activating/cleaving enzyme ADAM-17, significantly decreases the level of NICD and accumulation of NICD in the nucleus; exhibits cytotoxic acitviity…
View activity & pricesDC7923TAK-599 (ceftaroline fosamil)
TAK-599 (ceftaroline fosamil) is a cephalosporin with activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA).
View activity & pricesDC12131BF-227(E/Z)
BF 227 is a candidate for an amyloid imaging probe for PET, with a Ki of 4.3 nM for Aβ1-42 fibrils.
View activity & pricesDC8389Epacadostat (INCB024360)
Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM.
View activity & pricesDC7750UNC-0642
UNC0642 is a potent and selective G9a/GLP inhibitor, with an IC50 of less than 2.5 nM.
View activity & pricesDC5024MK-8776 (SCH 900776)
SCH900776 is a potent, selective and oral inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. It shows 50- and 500-fold selectivity over CDK2 andChk2, respectively.
View activity & pricesDC7266Rilpivirine(R 278474, TMC 278)
Rilpivirine (R278474; TMC278) is a type of anti-HIV medicine called a non-nucleoside reverse transcriptase inhibitor (NNRTI).
View activity & pricesDC1078AG-1478 (Tyrphostin AG-1478)
AG-1478 is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM.
View activity & pricesDC4200Fulvestrant
Fulvestrant is a potent Estrogen Receptor antagonist with an IC50 of 9.4 nM.
View activity & pricesDC7937LFM-A13
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
View activity & pricesDC7514TCS PIM-1 1
TCS PIM-1 1(sc-204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).TCS PIM-1 1 bound convincingly within the…
View activity & pricesDC60042YKP-3089
Cenobamate, a sodium channel blocker, enhances GABAergic transmission and has the potential to be a versatile CNS drug.
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