DC7620MS436
MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.
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Small Molecule Research Tools
2816 products · Page 5 of 59
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DC7620DC7169JW55
JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro…
View activity & pricesDC7027Glasdegib(PF-04449913)
Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM.
View activity & pricesDC3116RO-3306
Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
View activity & pricesDC1033S3I-201 (NSC-74859)
NSC 74859 is a selective Stat3 inhibitor with an IC50 of 86±33 μM.
View activity & pricesDC1106PCI-32765 (Ibrutinib)
Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
View activity & pricesDC8290(S)-PFI-2 HCl
Negative control of (R)-PFI 2 hydrochloride. Exhibits 500-fold lower activity in a SETD7 enzymatic assay (IC50 = 1 μM) compared to the active enantiomer.
View activity & pricesDC9698Staurosporine
Staurosporine is a potent and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively.
View activity & pricesDC8537AZ505
AZ505 is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
View activity & pricesDC8305Edoxaban
Edoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention in patients with atrial fibrillation, an elderly population that frequently receives aspirin (ASA) and/or nonsteroidal…
View activity & pricesDC5108BAY 59-7939 (Rivaroxaban)
Rivaroxaban is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
View activity & pricesDC5114Apixaban (BMS 562247-01)
Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
View activity & pricesDC8615L-685,458
L-685458 is a potent inhibitor of Amyloid β-Protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested.IC50 value: 17 nMTarget:…
View activity & pricesDC8039SP-420
SP-420 is a desferrithiocin analogue with iron-clearing efficiency with ICE value of 26.7; more potent than desferrithiocin.
View activity & pricesDC7084Nintedanib (BIBF 1120)
BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
View activity & pricesDC7468ML-323
ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
View activity & pricesDC7811Fexinidazole
Fexinidazole is an antiparasitic agent. It has activity against Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis, Entamoeba histolytica, Trypanosoma brucei, and Leishmania donovani. The biologically…
View activity & pricesDC7649PFI-3
PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
View activity & pricesDC7915UNC0321
UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.It was found that replacing the 5-carbon chain in…
View activity & pricesDC7527VE-822 (Berzosertib)
Berzosertib (VE-822) is an ATR inhibitor with a Ki value of less than 0.2 nM. It also inhibits ATM with a Ki of 34 nM.
View activity & pricesDC5154BKM120 (NVP-BKM120, Buparlisib)
NVP-BKM120 is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
View activity & pricesDC5142StemRegenin 1(SR-1)
StemRegenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
View activity & pricesDC28031AB928
A2aR/A2bR antagonist-1 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist with immunomodulatory activity[1].
View activity & pricesDC7004AR-A014418(GSK3β Inhibitor VIII)
AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor with an IC50 of 104 nM。
View activity & pricesDC7675BX-471（ZK 811752）
BX471 (ZK-811752) is a potent and selective non-peptide CCR1 antagonist with a Ki of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
View activity & pricesDC7680IM-12
IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.
View activity & pricesDC7006AZD-9291(Osimertinib)
Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
View activity & pricesDC7444kobe2602
kobe2602 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 149 ± 55…
View activity & pricesDC10834PF-06869206
PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.
View activity & pricesDC6305LY364947
LY-364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
View activity & pricesDC7186LGK-974
LGK974 is a potent and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM.
View activity & pricesDC6401Odanacatib (MK 0822)
Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.
View activity & pricesDC7200Motesanib Diphosphate (AMG-706)
Motesanib Diphosphate is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than…
View activity & pricesDC7197ML 161
Parmodulin 2 (ML161),a probe, is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 inhibits platelet aggregation induced by a PAR1 peptide agonist or by thrombin and…
View activity & pricesDC3107Momelotinib (CYT387,CYT-387)
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
View activity & pricesDC7420GNF-5
GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).IC50 Value: 0.22±0.1 uM (Wild type Abl)…
View activity & pricesDC7342Foretinib(XL880)
Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
View activity & pricesDC1068XL147 analogue(PI3K inhibitor X)
Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
View activity & pricesDC4103Dabrafenib Mesylate
Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively.
View activity & pricesDC7184Lcl-161
LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
View activity & pricesDC7177JNJ 38877605
JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
View activity & pricesDC7153CX6258
CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.
View activity & pricesDC7941PF-431396
PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.
View activity & pricesDC7395Dapivirine
apivirine(TMC 120, TMC 120 R147681) is a NNRTI for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates.
View activity & pricesDC8495PTC-209 hydrobromide
PTC-209 hydrobromide is a specific BMI-1 inhibitor with IC50 of 0.5 μM in both GEMS reporter and ELISA assays.
View activity & pricesDC5189SB-431542
SB-431542 is a potent and selective inhibitor of ALK5 with an IC50 value of 94 nM, and is also an inhibitor of TGF-β Receptor.
View activity & pricesDC7671UNC0379
UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 uM; selective over 15 other methyltransferases.UNC0379 is a synthetic small-molecule inhibitor that…
View activity & pricesDC5037BMS-536924
BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM.
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