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WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM . WT-161 also inhibits metallo-β-lactamase domain-containing protein?2 (MBLAC2) .
Choline hydroxide, 46 wt.% in water is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
WT1 Human Pre-designed siRNA Set A contains three designed siRNAs for WT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
EGFR WT/T790M-IN-1 (Compound 16h) is a dual EGFR WT and EGFR T790 inhibitor. EGFR WT/T790M-IN-1 can arrest the cell cycle in G2/M phase and induce apoptosis. EGFR WT/T790M-IN-1 has anti-cancer activity .
EGFR WT/T790M-IN-2 (Compound 7c) is a EGFR T790M/WT inhibitor with IC50 values of 0.08 and 0.13 μM, respectively. EGFR WT/T790M-IN-2 induces apoptosis by blocking the G0-G1 phase (apoptosis). EGFR WT/T790M-IN-2 has antitumor activity .
EGFR WT/T790M/L858R-IN-1 (compound 10d) is a potent EGFR inhibitor, with IC50s of 0.097, 0.280, and 0.051?μM for EGFR WT, EGFR T790M, and EGFR L858R, respectively. EGFR WT/T790M/L858R-IN-1 can be used for the research of cancer .
Mtb-IN-6 (Compound C10) is a Mycobacterium tuberculosis(Mtb) respiration inhibitor. Mtb-IN-6 can enhance the bactericidal activity of isoniazid (INH, HY-B0329). Mtb-IN-6 inhibits WTMtb with an IC50 of 25 µM .
HIV-1 integrase inhibitor 13 (Compound 15) is an inhibitor for HIV-1 integrase with an IC50 of 1.8 nM. HIV-1 integrase inhibitor 13 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 21 and 580 nM, respectively .
HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor with IC50 values of 23.6 and 307.5 nM for EGFR LR/TM/CS and EGFR WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research .
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
AT-130, a phenylpropenamide derivative, is a potent hepatitis B virus (HBV) replication non-nucleoside inhibitor. AT-130 inhibits the viral DNA synthesis with an EC50 of 0.13 μM. AT-130 inhibits both wt and mutant HBVs. AT-130 has anti-HBV activity in hepatoma cells .
RET-IN-16 is a potent and selective RET inhibitor with IC50s of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM and 8.86 nM for RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6 and RET-KIF5B, respectively. RET-IN-16 has anticancer effects .
HPK1-IN-33 (compound 21) is a potent Hematopoietic Progenitor Kinase 1 (HPK1) inhibitor with a Ki value of 1.7 nM. HPK1-IN-33 inhibits the produce of IL-2 with EC50s of 286, >10000 nM in Jurkat WT and Jurkat HPK1 KO cells, respectively .
LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkA G595R and TrkA G667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity .
RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF wt, and bRAF V600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF V600E mutation, respectively .
LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier .
LRRK2-IN-6 (compound 22) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-6 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-6 can cross the blood-brain barrier .
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .
HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) .
PDGFRα kinase inhibitor 2 (compound 1), an Imatinib (HY-15463) analogue, is a covalent and irreversible kinase inhibitor with IC50s of 6.95 μM, 2.45 μM, 1.39 μM for ABL1wt, KITwt, PDGFRRwt .
Choline hydroxide is a Choline hydrogen oxidized derivative and a strong organic base, can be used as the standard alkaline to adjust the pH of the medium. Choline is an orally active nutrient, serves as an important component of lecithin and sphingomyelin, promotes fat metabolism .
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2 WT and EGFR WT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer .
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
BCR-ABL-IN-7 (compound 4) is a WT and T315I mutant ABL kinases inhibitor. BCR-ABL-IN-7 effectively inhibits activities of WT and T315I mutant ABL kinases. BCR-ABL-IN-7 can be used for the research of chronic myeloid leukemia (CML) research .
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively .
GSK3532795 oxalate is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively .
GSK3532795 hydrochloride is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively .
GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively .
LRRK2-IN-12 (compound 1) inhibits the activity of LRRK2 G20195 (IC50=0.45 nM), LRRK2 WT (IC50=1.1 nM) and LRRK2 WT ADP-Glo (IC50=0.46 nM). LRRK2-IN-12 can be used for Alzheimer's Disease research .
EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research .
MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .
MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .
FLT3-IN-25 (compound 17) is a potent inhibitor of FLT3, with IC50s of 1.2 nM, 1.4 nM and 1.1 nM for FLT3-WT, FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-25 plays an important role in acute myeloid leukemia (AML) .
4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC50 value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity .
KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC50 values of 0.55 nM, 25.1 nM and 5.4 nM against TRK WT, TRK G595R and TRK G667C, respectively. TRK-IN-2 shows antiproliferative activity with IC50 values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKA WT, Ba/F3-ETV6-TRKB WT, Ba/F3-LMNA-TRK G595R and Ba/F3-LMNA-TRKA G667C, respectively .
CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe .
PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively .
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ～40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ～250 and ～500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia .
SILA-123 is a FLT3 inhibitor (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM). SILA-123 inhibits FLT3 phosphorylation and downstream signaling pathways, leading to apoptosis by arresting cell cycle progression at the G0/G1 phase. SILA-123 can be used in the study of acute myeloid leukemia .
B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
Acoramidis (AG10) is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) is used in the study for transthyretin amyloidosis .
Acoramidis (AG10) hydrochloride is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) hydrochloride is used in the study for transthyretin amyloidosis .
HIV-1 inhibitor-28 (compound 14j2) is a highly potent and selective HIV-1 inhibitor with an EC50 of 58 nM for WT HIV-1 strain and an IC50 of 3.37 μM for HIV-1 WT reverse transcription (RT). HIV-1 inhibitor-28 exhibits relatively low cytotoxicity in MT-4 cells (CC50 = 38.6 μM). HIV-1 inhibitor-28 can be used for researching AIDS .
5-Aza-7-deazaguanine is a substrate for wild-type (WT) E. colipurine nucleoside phosphorylase and its Ser90Ala mutant in the synthesis of base-modified nucleosides .
ient S. Tm and hyperpermeable Escherichia coli. The potencies against WT strains of E. coli, Acinetobacter baumannii, and Burkholderia cenocepacia are also improved considerably (up to >128-fold) with the outer-membrane permeabi
Cyclobendazole is a benzimidazole derivative against protozoan parasites. Cyclobendazole shows in vitro activities against Trichomonas vaginalis (30236) and Giardia lamblia (wt), with IC50 values of 1.1 and 0.047 μg/mL, respectively .
3-Azaspiro[5.5]undecane (4,4-Pentamethylenepiperidine) hydrochloride is an inhibitor targeting the WTinfluenza A virus M2 (A/M2), with an IC50 of 1 μM .
ERK2-IN-3 (compound 2) is a inhibitor of ERK2, and inhibits Erk2 WT and Erk2 DS1 activation loop phosphorylation, with IC50 of 5 μM and 42 nM, respectively .
FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM) .
c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC50 of 246.6 nM against wt-AR, and is also an AR degrader with a DC50 of 2.84 μM .
CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively .
EGFR-IN-75 is an EGFR WT and EGFR T790M inhibitor with IC50 values of 0.28 μM and 5.02 μM, respectively. EGFR-IN-75 shows anticancer and antioxidant activity .
T-1-PMPA is a potent EGFR inhibitor with apoptotic properties. T-1-PMPA effectively inhibits EGFR WT and EGFR 790m, with IC50 values of 86 nM and 561.73 nM, respectively .
FRF-06-057 is an ATP-allosteric EGFR inhibitor against wild-type and mutant EGFR, with IC50s of 17 nM (LR/TM), 29 nM (LR/TM/CS), 220 nM (LR), > 1000 nM (WT) respectively .
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer .
FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML) .
HIV-1 inhibitor-44 (compound 11l) is a HIV-1 reverse transcriptase inhibitor. HIV-1 inhibitor-44 shows inhibitory activity against wild-type HIV-1 strain with an EC50 value of 0.209 μM .
dCeMM1 is a RBM39 glue degrader. dCeMM1 shows functions by re-directing the activity of the CRL4 DCAF15 ligase. dCeMM1 decreases the expression of RBM39 levels in WT KBM7 cells .
AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2 R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2 WT with IC50 of 190±8.1 nM.
ZN-A-1041 inhibits HER2 in BT474 cell and wt-EGFR in H838 cells, with IC50s of 9.5 nM and 12 μM respectively. ZN-A-1041 can be used for research of cancer and inflammation .
EZH2-IN-19 (conpound N40) is a potent inhibitor of enhancer of zeste homolog 2 (EZH2) WT, with the IC50 of 0.32 nM. EZH2-IN-19 plays an important role in cancer research .
ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
HIV-1 inhibitor-32 (compound 3c) is a potent HIV-1 inhibitor with an IC50 value of 34 nM for WT HIV-1. HIV-1 inhibitor-32 can be used for researching AIDS .
JMF4073 is a thymidylate (TMP) and cytidylate (CMP) kinases inhibitor with IC50s of 0.16 μM and 0.17 μM, respectively. JMF4073 eliminates wild-type (WT)-Bcr-Abl-transformed myeloid cells in vitro and in vivo .
Dacomitinib metabolite M1/2 is a potent inhibitor of both wild-type (WT) EGFR and the T790M mutation, demonstrating significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC).
Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3β WT (1 h preincubation) and GSK-3β C199A (1 h preincubation), respectively.
T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).
B-Raf IN 15 (Compound 7) is a BRAF inhibitor. B-Raf IN 15 inhibits BRAF WT and BRAF V600E with IC50s of 2.0 and 0.8 μM. B-Raf IN 15 can be used for the research of cancer .
MS154 is a first-in-class E3 ligase cereblon-recruiting EGFR degrader with Kds of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutants. MS154 potently inhibits cell proliferation in lung cancer cells .
EZH2-IN-18 (compound 9e) is a potent inhibitor of enhancer of zeste homologue 2 (EZH2WT) , with the IC50 of 1.01 nM. EZH2-IN-18 shows inhibition in proliferation and induction in apoptosis in tumor cells .
Olafertinib is a third-generation EGFR TKI, with GI50 values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFRWT), respectively. Olafertinib has the potential for NSCLC research .
RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .
Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity .
PF-06447475 is a highly potent, selective, brain penetrant LRRK2 kinase inhibitor with IC50 values of 3 nM and 11 nM for WT LRRK and G2019S LRRK2, respectively. PF-06447475 can be used for parkinson's disease (PD) research .
Quinine hydrochloride dihydrate (Qualaquin) is an orally active and can be used in anti-malarial studies. Quinine hydrochloride dihydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
Quinine is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
RO-0335 is a novel and potent diphenylether nonnucleoside reverse transcriptase inhibitor(NNRTI). RO-0335 inhibits Wt HIV-1 with an IC50 of 1.1 nM and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates .
T-1-DOCA ia a EGFR inhibitor, with the IC50 of 56.94 and 269.01?nM for EGFR WT and EGFR T790M, respectively. T-1-DOCA can induces cell apoptosis of HCT-116 cells .
Quinine (hydrochloride) is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine (hydrochloride) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR WTIC50=281 nM, c-MET IC50=205 nM, B-RAF WTIC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR T790MIC50=69 nM and B-RAF V600EIC50=83 nM) .
XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis .
limertinib (ASK120067) diTFA is a potent and orally active inhibitor of EGFR T790M (IC50: 0.3 nM) with selectivity over EGFRWT (IC50: 6.0 nM). limertinib diTFA is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .
HER2-IN-20 (compound 32) is a potent and selective HER2 WT and HER2 YVMA inhibitor with IC50 values of 49, 42 nM, respectively. HER2-IN-20 has the potential for the research of non-small cell lung cancer (NSCLC) .
AZSMO-23 is a potent hERG K + channel activator. AZSMO-23 activats WT hERG pre-pulse and tail current with EC50 values of 28.6, 11.2 µM, respectively. AZSMO-23 has the potential for the research of long QT syndrome .
Quinine hemisulfate hydrate, an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine hemisulfate hydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV, with an IC50 of 169 μM .
CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability .
Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine dihydrochloride is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
EGFR/HER2-IN-15, a dihydropyrimidine, is a potent EGFR/HER2 inhibitor. EGFR/HER2-IN-15 significantly inhibits EGFR wt activity with an IC50 of 37.21 nM. EGFR/HER2-IN-15 has anticaner effects .
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAF V600E and B-RAF WT, respectively .
(R,R)-GSK321 is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. (R,R)-GSK321 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity .
RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC50s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research .
FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4 WT, FGFR3, FGFR4 V550L, FGFR2 and FGFR1, respectively .
LRRK2-IN-8 is a LRRK2 inhibitor. LRRK2-IN-8 inhibits LRRK2 (wt) and LRRK2 (G2019) with IC50s lower than 10 nM, and inhibits TYK2 and NUAK1 with IC50s of 10-100 nM .
MK-4965 is a nonnucleoside reverse transcriptase inhibitor (NNRTI). MK-4965 displays excellent activities against not only HIV-1 wild-type (WT) virus but also against a broad panel of NNRTI-resistant viruses and can be used for the research of HIV-1 infection .
Lysyl hydroxylase 2-IN-2 (compound 13) is a potent Lysyl hydroxylase 2 (LH2) inhibitor, with the IC50 of approximately 500 nM. Lysyl hydroxylase 2-IN-2 inhibits the migration in 344SQ WT cells, but not impedes the migration of the same cell line with an LH2 knockout cells .
limertinib (ASK120067) is a potent and orally active inhibitor of EGFR T790M (IC50:0.3 nM) with selectivity over EGFR WT (IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .
Cabamiquine (DDD107498) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. Cabamiquine inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2 .
Quinine hemisulfate is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine hemisulfate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM . Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias .
Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis .
Cabamiquine (DDD107498) succinate is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. Cabamiquine succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2 .
Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively .
DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy .
RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research .
B-Raf IN 11 (ZINC72115182) is a selective B-Raf V600E inhibitor (IC50=76 nM), shows selectivity for
B-Raf V600E over B-Raf WT with selectivity of 3.1-fold. B-Raf IN 11 can be used in colorectal cancer research
pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively .
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFR L858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFR WT (IC50 >1.0 μM) .
SLEC-11 acts as a potential synthetic lethal lead for the research of gastric cancer. AL-GDa62 shows EC50 of 12.2 μM and 8.2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1 -/- .
AL-GDa62 acts as a potential synthetic lethal lead for the research of gastric cancer. AL-GDa62 shows EC50 of 3.2 μM and 2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1 -/- .
EGFR-IN-30 is a potent EGFR inhibitor with IC50s of 1-10 nM, <1 nM for EGFR (WT), EGFR (L858R/T790M/C797S), respectively. EGFR-IN-30 has potential for cell proliferative diseases, such as cancer research .
VRT-534 targets connexin 26 (Cx26). Vrt-534 exhibits dose-responsive binding to recombinant WT Cx26 and mutant Cx26 K188N with EC50 value of 19 μM and 5 μM, respectively. Vrt-534 can be used in research related to hearing impairment .
4 '-DTMP is a DHFR inhibitor with Ki of 5.1 nM (DHFR WT) and 34.3 nM (DHFR L28R), respectively. 4 '-DTMP carries a polar modification that induces additional local interactions with the enzyme. In particular, the hairpin structure on the M20 ring is related to the internal communication of the DHFR. 4 '-DTMP has potential inhibition of E.coli .
STAT3-IN-4 (compound B9) is a STAT3 inhibitor with Kd values for STAT3 (I634S/Q635G) and WT are 22.75 and 4.59 μM, respectively. STAT3-IN-4 can inhibit the proliferation of tumor cells .
RET-IN-27 (compound 20p) is a potent inhibitor of RET, with IC50s of 3.6 nM, 0.1 nM, 2.1 nM, 0.3 nM for RET WT, RET V804L, RET V804M, RET M918T, respectively. RET-IN-27 plays an important role in cancer research .
SMIP34 is a PELP1 inhibitor. SMIP34 binds to PELP1 with a Kd of 37.4 μM. SMIP34 inhibits cancer cell proliferation and tumor progression. SMIP34 can be used for breast cancer research, and is active against wild-type (WT), mutant (MT) ER + and therapy-resistant (TR)-ER + breast cancer .
Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1 WT and Abl1 T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively . Anticancer activity .
RET-IN-14 (compound 49) is a potent RET inhibitor with IC50s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research
ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS .
PAN endonuclease-IN-1 (Compound 23) is a potent PAN endonuclease inhibitor, with Kd values of 277 μM, 384 μM and 328 μM for WT, I38T and E23K PAN endonucleases, respectively. The RNA-dependent RNA polymerase acidic N-terminal (PAN) endonuclease, a critical component of influenza viral replication machinery, is an antiviral target .
Selpercatinib (Standard) is the analytical standard of Selpercatinib. This product is intended for research and analytical applications. Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity .
Quinine (Standard) is the analytical standard of Quinine. This product is intended for research and analytical applications. Quinine is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
BRD5080 is a potent GPR65 positive allosteric modulator. BRD5080 induces GPR65-dependent cAMP production. BRD5080 exhibits a robust induction of cAMP activity and recruits G protein for the WT and variant hGPR65 as well as for the mouse ortholog. BRD5080 has the potential for autoimmune and inflammatory diseases research .
ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression .
Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively .
Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis .
SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity .
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity .
MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .
HIV-1 inhibitor-55 (compound 4d) inhibits WT HIV-1 with an EC50 value of 8.6 nM. HIV-1 inhibitor-55 also shows inhibitory potency against single and double HIV-1 mutants. HIV-1 inhibitor-55 can be used for the research of virus infection .
Quinine sulfate hydrate (2:1:4) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate hydrate (2:1:4) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM .
EGFR-IN-109 (compound 4) is an EGFR inhibitor, with the IC50 values of 25.8 and 182.3 nM for EGFR WT and EGFR T790M, respectively. EGFR-IN-109 arrests the cancer cells’ growth at the G2/M phase and induces both early and late apoptosis. EGFR-IN-109 can be used in cancer research .
Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC50 of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC50 of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats .
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines .
SR-717 free acid is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 free acid is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity .
Tafamidis-d3 is deuterium labeled Tafamidis. Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis[1].
TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALK WT and ALK L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases .
EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC50 values of 70 nM and 3.9 nM against EGFR WT and EGFR L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity .
BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl WT and Bcr-Abl T3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells .
HIV-1 inhibitor-54 is a potent HIV-1 inhibitor. HIV-1 inhibitor-54 has anti-HIV activity in MT-4 cells against WT HIV-1 (strain IIIB) with an EC50 value of 0.032 μM. HIV-1 inhibitor-54 can be used for the research of virus infection .
TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC50 value of 42 μM .
EGFR-IN-87 is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 has IC50 value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 can be used for cancer diseases research .
Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-penetrant, EGFR inhibitor (IC50s: 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research .
YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7 WT and Cdk7 as, although Cdk7 as is relatively resistant to this compound as well .
I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents .
Quinine (hydrochloride dihydrate) (Standard) is the analytical standard of Quinine (hydrochloride dihydrate). This product is intended for research and analytical applications. Quinine hydrochloride dihydrate (Qualaquin) is an orally active and can be used in anti-malarial studies. Quinine hydrochloride dihydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM .
Quinine (dihydrochloride) (Standard) is the analytical standard of Quinine (dihydrochloride). This product is intended for research and analytical applications. Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine dihydrochloride is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM .
K-Ras-IN-1 is a small molecule K-Ras inhibitor. K-Ras-IN-1 binds to K-Ras (WT), K-Ras (G12D), K-Ras (G12V), and H-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. K-Ras-IN-1 is promising for research of pancreatic, colon and lung cancer .
Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research .
Amiodarone-d4 (hydrochloride) is the deuterium labeled Amiodarone hydrochloride. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM[1]. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts[2]. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias[1].
EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers .
UPCDC-30245 is an allosteric p97 inhibitor with an IC50 of approximately 27 nM . UPCDC-30245 inhibits the p97 mutant N660K similar to wild type (WT; IC50=300 nM) and shows 3-fold resistance for p97 mutant T688A . UPCDC-30245 can be used in the research of cancer .
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .
LJ-4517 is a potent A2AAR antagonist, with a Ki of 18.3 nM. LJ-4517 is potent in displacing the binding of [ 3H]ZM241385 (HY-19532) at WT A2AAR . LJ-4517 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
HIV-1 inhibitor-59 (Compound I-5b) is a HIV-1 inhibitor, with EC50s of 5.62-171 nM against the wild-type (WT) and mutant HIV-1 strains. HIV-1 inhibitor-59 has moderate RT enzyme inhibitory activity (IC50: 0.094-12.0 μM) .
Amiodarone (hydrochloride) (Standard) is the analytical standard of Amiodarone (hydrochloride). This product is intended for research and analytical applications. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM . Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias .
IP2 is an immunomodulatory agent. IP2 increases PTP (Pioneer Translation Product)-derived antigen presentation in cancer cells. IP2 shows non-cytotoxic for cancer cells. IP2 induces tumor growth defects in mouse .
MS-II-124 is an effective and selective NLRP3 inhibitor (IC50=0.12 μM) with anti-inflammatory and immunomodulatory activities, which can be used in the research of acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) .
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase .
TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .
EGFR-IN-81 (Compound 10i) is an EGFR inhibitor. EGFR-IN-81 inhibits EGFR WT and L858R/T790M with IC50s 4.38 nM and 5.69 nM. EGFR-IN-81 has cytotoxic activity against MCF-7 and HCT116 cells with of 2.07 μM and 6.72 μM respectively .
EGFR-IN-136 (compound 21v) is a potent EGFR inhibitor with IC50 values of 20.2, 1.2, 2.3, 12.5 nM for EGFR WT, EGFR LR/TM, EGFR 19D/TM/CS, EGFR LR/TM/CS, respectively. EGFR-IN-136 shows antiproliferative activity. EGFR-IN-136 shows antitumor activity and has the potential for the research of NSCLC .
N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively . N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM .
RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects .
HIV-1 inhibitor-14 (compound 14b) is a highly potent and broad-spectrum HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor with an EC50 of 0.14 μM for HIV-1 RT. HIV-1 inhibitor-14 has inhibitory activity against HIV-1 WT and resistant strains with EC50s of 5.79 ~ 28.3 nM .
LRRK2/NUAK1/TYK2-IN-1 (conpound 226) shows inhibitory activity toward LRRK2 (Wt), LRRK2 (G2019), TYK2 and NUAK1, with IC50 values lower than 10 nM. LRRK2/NUAK1/TYK2-IN-1 can be used for autoimmune disease research .
RET-IN-23 (compound 17) is a potent and orally active RET inhibitor with IC50 values of 1.32, 2.50, 6.54, 1.03, 1.47 nM for RET-WT, RET-CCDC6, RET-V804L, RET-V804M, RET-M918T, respectively. RET-IN-23 shows anti-tumor activity .
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
DHFR-IN-20 (Compound LA1) is a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor, with Kis of 0.16, 0.30, 6.6 nM for PfDHFR-WT, PfDHFR-QM, HsDHFR. DHFR-IN-20 has antimalarial activities (IC50: 1.4 nM and 1.6 μM for P. falciparum carrying the wild-type (TM4/8.2) and the quadruple mutant (V1/S) PfDHFR enzyme .
DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively . DB008 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
Islatravir (MK-8591) is a potent anti-HIV-1 agent, acting as a nucleoside reverse transcriptase inhibitor, with EC50s of 0.068 nM, 3.1 nM and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively. Islatravir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases .
MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase .
HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability .
UBP141 is a GluN2C/2D (NR2C/2D)-preferring receptor antagonist, with Kds of 2.8, 4.2, 14.2, and 19.3 μM for NMDA receptor subtypes: GluN2C, 2D, 2A, and 2B, respectively. UBP141 can induce potent motor impairment in WT mice .
Pralsetinib (Standard) is the analytical standard of Pralsetinib. This product is intended for research and analytical applications. Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively .
Quinine (sulfate hydrate) (Standard) is the analytical standard of Quinine (sulfate hydrate). This product is intended for research and analytical applications. Quinine sulfate hydrate (2:1:4) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate hydrate (2:1:4) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM .
Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-Abl WT and Bcr-Abl T315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies .
H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations .
ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers .
HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM .
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .
PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells .
EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively .
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
ML786 is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers .
S-312-d (S-(+)-S-312-d) is a calcium channel blocker with the activity of protecting the kidney from ischemic acute renal failure. S-312-d (0.01-0.1mg/kg b.wt. iv) administered before ischemia has a dose-dependent protective effect on ischemia-induced renal damage, improves the survival rate of ischemic rats, and reduces renal cortical edema and the increase in renal tissue calcium content.
Tubulin polymerization-IN-73 (Compound 37) is an inhibitor for microtubule polymerization with an IC50 of 1.8 μM. Tubulin polymerization-IN-73 arrests the cell cycle at G2/M phase, induces apoptosis in A549 cell, inhibits the proliferation of A549 WT and A549/T resistant cell with IC50 of 0.023 μM and 0.057 μM. Tubulin polymerization-IN-73 exhibits antitumor efficacy in mouse model .
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
10-Undecenoic acid zinc salt is a RNA-dependent RNA polymerase (RdRp) inhibitor, with an IC50 of 1.13, 21.33 and 1.79 μM for WT-RdRp, D535ARdRp and D692A-RdRp, respectively. 10-Undecenoic acid zinc salt reduces infectious virus yield in Huh7 cells with an EC50 of 7.43 μM. 10-Undecenoic acid zinc salt has anti-infective and anti-fungal activity. 10-Undecenoic acid zinc salt can be used for the research of Zika virus (ZIKV) .
BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines .
HIV-1 inhibitor-22 (compound 11a) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 3.63 μM for HIV-1 RT. HIV-1 inhibitor-22 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 0.304 μM and 0.201 μM, also has low cytotoxicity (CC50 > 227 μM)
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
XL01126 is a potent LRRK2 PROTAC (DC50: 14 nM (G2019S LRRK2) and 32 nM (WTLRRK2)) composed of the VHL ligand VH 101, thiol (HY-47851, blue part) and the LRRK2 inhibitor HG-10-102-01 (HY-13488, red part). XL01126 crosses the blood-brain barrier and is used as a degradation probe in Parkinson's disease research. XL01126 can be used to study the non-catalytic and framework functions of LRRK2 .
EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research .
HIV-1 inhibitor-74 (compound 10c) is a potent HIV-1 inhibitor with an EC50 value of 0.0047 µM for HIV-1 IIIB. HIV-1 inhibitor-74 shows cytotoxicity. HIV-1 inhibitor-74 inhibits WT HIV-1 RT activity with an IC50 value of 0.134 µM. HIV-1 inhibitor-74 shows broad-spectrum anti HIV-1 activity .
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .
Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells .
GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WTL. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties .
HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety .
HIV-1 inhibitor-21 (compound 9b) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC50 value of 0.55 μM for HIV-1 RT. HIV-1 inhibitor-21 has antiretroviral activity against HIV-1 WT and K103N strains with EC50s of 12.7 nM and 10.4 nM, and has relatively low cytotoxicity (MT-4 cells CC50 =10.2 μM) .
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability .
ALK-IN-21 (Compound B10), a potent ALK inhibitor for ALKG1202R mutation, exhibits remarkable enzymatic inhibitory potency with IC50 values of 4.59 nM, 2.07 nM and 5.95 nM toward ALK WT, ALK L1196M and ALK G1202R, respectively. ALK-IN-21 efficiently inhibits the proliferation of ALK-positive Karpas299 and H2228 cells both with IC50 values of 0.07 μM. ALK-IN-21 can be used for the research of anaplastic large cell lymphoma .
Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC50s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC50s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively .
Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells .
AKE-72 (compound 5) is a potent inhibitor of Pan-BCR-ABL. AKE-72 inhibits BCR-ABL WT, BCR-ABL T315, BCR-ABL E255K, BCR-ABL F3171, BCR-ABL H396P and BCR-ABL Q252H with IC50s of < 0.5, 9, 8.98, 3.12, < 1.0 and 3.88 nM, respectively. AKE-72 has anti-leukemic activity against K-562 cell line .
AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis .
CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML) .
BCR-ABL-IN-6 (9h) is a selective Bcr-Abl kinase inhibitor with IC50s of 4.6 and 227 nM for Bcr-Abl WT and Bcr-Abl T3151 respectively. BCR-ABL-IN-6 inhibits Bcr-Abl kinase with strong affinity inside the cells with an EC50 of 14.6 nM. BCR-ABL-IN-6 is an imatinib derivative which can be used for research of chronic myelogenous leukemia . BCR-ABL-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity .
BA6b9 is an allosteric inhibitor of SK4 channels that targets the CaM–PIP2-binding domain with a IC50 value of 8.6 µM (WT SK4). BA6b9 inhibits SK4 channels by interacting with two specific residues, Arg191 and His192 in the S4–S5 linker. BA6b9 significantly prolongs atrial and atrioventricular effective refractory period (ERP) and reduces atrial fibrillation (AF) induction in rat isolated hearts, which has the potential to be used for the research of arrhythmia .
Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFRwt, EGFRL858R/T790M, EGFRL858R and EGFRT790M, respectively .
BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .
ATPA is a selective glutamate receptor GluR5 activator with EC50s of 0.66, 9.5, 1.4, 23, 32, 18, and 14 μM for GluR5wt, GluR5(S741M), GluR5(S721T), GluR5(S721T, S741M), GluR5(S741A), GluR5(S741L), and GluR5(S741V), respectively .
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively .
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
(S,R)-GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
10-Undecenoic acid (zinc salt) (Standard) is the analytical standard of 10-Undecenoic acid (zinc salt). This product is intended for research and analytical applications. 10-Undecenoic acid zinc salt is a RNA-dependent RNA polymerase (RdRp) inhibitor, with an IC50 of 1.13, 21.33 and 1.79 μM for WT-RdRp, D535ARdRp and D692A-RdRp, respectively. 10-Undecenoic acid zinc salt reduces infectious virus yield in Huh7 cells with an EC50 of 7.43 μM. 10-Undecenoic acid zinc salt has anti-infective and anti-fungal activity. 10-Undecenoic acid zinc salt can be used for the research of Zika virus (ZIKV) .
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC50 less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC50: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch .
(1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
NX-2127 (compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells . NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).
EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values < 10 nM) under hypoxic condition .
Maleic Acid (Standard) is the analytical standard of Maleic Acid. This product is intended for research and analytical applications. Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes.
IC50 & Target: GAD .
In Vitro: The MICs of WT 10403S for the acids (e.g., Maleic Acid) are 34 mM, 25 mM, 31 mM and 30 mM which correspond to pH values prior to growth of 4.84, 5.14, 5.32 and 5.02 respectively. Of all compounds tested, Maleic Acid is the least inhibitory despite acting at a lower pH (4.84). The most acid resistant (10403S) and the weakest (EGD-e) strain are challenged with 8.6 mM and 4.3 mM of each organic acid at pH 3 and 3.3 respectively. On both strains, Maleic Acid is the most bactericidal .
EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity .
EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR L858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFR WT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR L858R/T790M/C797S with an IC50 of 0.052 μM .
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .
JH-131e-153, a diacylglycerol (DAG)-lactone, is a small molecule activator of Munc13-1, targeting the C1 domain. The activation sequence of JH-131e-153 on Munc13-1 is WT>I590≈R592A≈W588A. The C1 domain of Munc13-1 and protein kinase C (PKC) are homologous in sequence and structure. The activation sequence of JH-131e-153 on Munc13-1 and PKC was PKCα>Munc13-1>PKCε. JH-131e-153 regulates neuronal processes through Munc13-1 and can be further used in the study of neurodegenerative diseases .
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
Choline hydroxide, 46 wt.% in water is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
BRC4wt (BRC4 repeat motif) is part of the BRACA2 tumor suppressor protein, which exhibits inhibitory activity against interaction of the BRACA2 protein with RAD51, and is involved in the repair of DNA damage .
Quazomotide is a WT1 class II peptide epitope with sequences of RSDELVRHHNMHQRNMTKL. Quazomotide stimulates a peptide-specific CD4(+) response, to recognize WT1(+) tumor cells. Quazomotide is an immunological agent for active immunization, as well as an antineoplastic agent .
Grisnilimab (WT1), a IgG2a monoclonal antibody anti-CD7, is a tumor suppressor involved in the etiology of Wilms' tumor. Grisnilimab regulates the transcription of multiple target genes and may participate in the post-transcriptional processing of RNA .
Quinine hydrochloride dihydrate (Qualaquin) is an orally active and can be used in anti-malarial studies. Quinine hydrochloride dihydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
Quinine is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
Quinine hemisulfate hydrate, an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine hemisulfate hydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV, with an IC50 of 169 μM .
Quinine sulfate hydrate (2:1:4) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate hydrate (2:1:4) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM .
Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine dihydrochloride is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
Quinine hemisulfate is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine hemisulfate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
Quinine (Standard) is the analytical standard of Quinine. This product is intended for research and analytical applications. Quinine is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM .
Quinine (hydrochloride dihydrate) (Standard) is the analytical standard of Quinine (hydrochloride dihydrate). This product is intended for research and analytical applications. Quinine hydrochloride dihydrate (Qualaquin) is an orally active and can be used in anti-malarial studies. Quinine hydrochloride dihydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM .
Quinine (dihydrochloride) (Standard) is the analytical standard of Quinine (dihydrochloride). This product is intended for research and analytical applications. Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine dihydrochloride is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM .
Quinine (sulfate hydrate) (Standard) is the analytical standard of Quinine (sulfate hydrate). This product is intended for research and analytical applications. Quinine sulfate hydrate (2:1:4) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate hydrate (2:1:4) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM .
10-Undecenoic acid zinc salt is a RNA-dependent RNA polymerase (RdRp) inhibitor, with an IC50 of 1.13, 21.33 and 1.79 μM for WT-RdRp, D535ARdRp and D692A-RdRp, respectively. 10-Undecenoic acid zinc salt reduces infectious virus yield in Huh7 cells with an EC50 of 7.43 μM. 10-Undecenoic acid zinc salt has anti-infective and anti-fungal activity. 10-Undecenoic acid zinc salt can be used for the research of Zika virus (ZIKV) .
10-Undecenoic acid (zinc salt) (Standard) is the analytical standard of 10-Undecenoic acid (zinc salt). This product is intended for research and analytical applications. 10-Undecenoic acid zinc salt is a RNA-dependent RNA polymerase (RdRp) inhibitor, with an IC50 of 1.13, 21.33 and 1.79 μM for WT-RdRp, D535ARdRp and D692A-RdRp, respectively. 10-Undecenoic acid zinc salt reduces infectious virus yield in Huh7 cells with an EC50 of 7.43 μM. 10-Undecenoic acid zinc salt has anti-infective and anti-fungal activity. 10-Undecenoic acid zinc salt can be used for the research of Zika virus (ZIKV) .
Maleic Acid (Standard) is the analytical standard of Maleic Acid. This product is intended for research and analytical applications. Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes.
IC50 & Target: GAD .
In Vitro: The MICs of WT 10403S for the acids (e.g., Maleic Acid) are 34 mM, 25 mM, 31 mM and 30 mM which correspond to pH values prior to growth of 4.84, 5.14, 5.32 and 5.02 respectively. Of all compounds tested, Maleic Acid is the least inhibitory despite acting at a lower pH (4.84). The most acid resistant (10403S) and the weakest (EGD-e) strain are challenged with 8.6 mM and 4.3 mM of each organic acid at pH 3 and 3.3 respectively. On both strains, Maleic Acid is the most bactericidal .
Wilms tumor protein (WT1) is a key transcription factor that critically regulates cell development and survival by binding to 5'-GCG(T/G)GGGCG-3'. It oversees target genes such as erythropoietin (EPO) and is critical for the development of the genitourinary system. Wilms tumor protein/WT1 Protein, Human (His-SUMO) is the recombinant human-derived Wilms tumor protein/WT1 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag. The total length of Wilms tumor protein/WT1 Protein, Human (His-SUMO) is 449 a.a., with molecular weight of ~65.2 kDa.
HLA-A*0201 MAGE-A4 Complex Protein, a member of the major histocompatibility complex (MHC) class I family, is highlighted. Additionally, the Chimeric HLA-A*0201 WT-1 Complex Tetramer is recognized within the MHC class I family. HLA-A*0201 WT-1 Complex Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing human-derived HLA-A*0201 WT-1 Complex protein, expressed by HEK293 , with C-Avi, C-His labeled tag. HLA-A*0201 WT-1 Complex Protein, Human (HEK293, His-Avi), has molecular weight of 52-60 kDa.
HLA-A*0201 WT-1 complex Protein, Human (HEK293, His) is the recombinant human-derived HLA-A*0201 WT-1 complex protein, expressed by HEK293 , with C-10*His labeled tag. , has molecular weight of 55-60 kDa.
LacI, the lactose operon repressor, regulates lactose metabolism by binding to the operator region and repressing gene transcription. The presence of the inducer, allolactose, alters its binding affinity, derepressing the operon. As a homotetramer, LacI finely tunes lactose metabolism, orchestrating regulatory mechanisms in response to the cellular environment. LacI WT Protein, E.coli (His) is the recombinant E. coli-derived LacI WT protein, expressed by E. coli , with N-10*His labeled tag. The total length of LacI WT Protein, E.coli (His) is 360 a.a., with molecular weight of approximately 42 kDa.
Ebola virus Glycoprotein/GP Protein is pivotal in viral entry, serving as the receptor-binding subunit.In later infection stages, GP1 down-regulates crucial host cell surface molecules, including integrins like ITGA1-6, disrupting adhesion and potentially causing blood vessel integrity disruption.GP1 interacts with host TLR4, stimulating monocyte differentiation, leading to T-lymphocyte bystander death.It down-regulates natural killer cell function, counters BST2/tetherin, cooperates with VP40 for NF-kappa-B activation, acts as an antibody decoy, and induces cytokine transcription in host macrophages and dendritic cells through TLR4 activation.Ebola virus Glycoprotein/GP Protein (QDA39862, HEK293, His) is the recombinant Virus-derived Ebola virus Glycoprotein/GP protein, expressed by HEK293 , with C-His labeled tag.
HLA-A*0201 MAGE-A4 Complex Protein, a member of the major histocompatibility complex (MHC) class I family, is highlighted. Additionally, the Chimeric HLA-A*0201 WT-1 Complex Tetramer is recognized within the MHC class I family. HLA-A*0201 WT-1 Complex Protein, Human (Biotinylated, HEK293, His-Avi) is a recombinant protein dimer complex containing human-derived HLA-A*0201 WT-1 Complex protein, expressed by HEK293 , with C-Avi, C-His labeled tag. HLA-A*0201 WT-1 Complex Protein, Human (Biotinylated, HEK293, His-Avi), has molecular weight of 55-60 kDa.
HLA-A*0201 MAGE-A4 Complex Protein, a member of the major histocompatibility complex (MHC) class I family, is highlighted. Additionally, the Chimeric HLA-A*0201 WT-1 Complex Tetramer is recognized within the MHC class I family. HLA-A*0201 WT-1 Complex Tetramer Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing human-derived HLA-A*0201 WT-1 Complex Tetramer protein, expressed by HEK293 , with C-Avi, C-His labeled tag. HLA-A*0201 WT-1 Complex Tetramer Protein, Human (HEK293, His-Avi), has molecular weight of 260-265 kDa.
HLA-A*0201 MAGE-A4 Complex Protein, a member of the major histocompatibility complex (MHC) class I family, is highlighted. Additionally, the Chimeric HLA-A*0201 WT-1 Complex Tetramer is recognized within the MHC class I family. Chimeric HLA-A*0201 WT-1 Complex Protein, Human&Mouse (HEK293, His-Avi) is the recombinant mouse-derived Chimeric HLA-A*0201 WT-1 Complex protein, expressed by HEK293 , with C-Avi, C-His labeled tag. Chimeric HLA-A*0201 WT-1 Complex Protein, Human&Mouse (HEK293, His-Avi), has molecular weight of 51-60 kDa.
HLA-A*0201 MAGE-A4 Complex Protein, a member of the major histocompatibility complex (MHC) class I family, is highlighted. Additionally, the Chimeric HLA-A*0201 WT-1 Complex Tetramer is recognized within the MHC class I family. Chimeric HLA-A*0201 WT-1 Complex Tetramer Protein, Human&Mouse (HEK293, His-Avi) is the recombinant mouse-derived Chimeric HLA-A*0201 WT-1 Complex Tetramer protein, expressed by HEK293 , with C-Avi, C-His labeled tag. Chimeric HLA-A*0201 WT-1 Complex Tetramer Protein, Human&Mouse (HEK293, His-Avi), has molecular weight of 260-265 kDa.
The Ebola virus NP/nucleoprotein is critical for viral genome protection and replication, forming a helical capsid to protect the genome.The VP35 interaction stabilizes the monomeric NP, maintaining solubility until replication triggers cooperative binding to viral RNA.Ebola virus NP/Nucleoprotein Protein (His) is the recombinant Virus-derived Ebola virus NP/Nucleoprotein protein, expressed by E.coli , with N-His labeled tag.
Ebola virus glycoproteins (GPs) play a key role in the virus entry process, with GP1 serving as the receptor-binding subunit and GP2 for membrane fusion.GP downregulates host cell surface molecules, disrupts adhesion and may lead to disruption of vascular integrity.Ebola virus Glycoprotein/GP Protein (AHX24649, sf9, His) is the recombinant Virus-derived Ebola virus Glycoprotein/GP protein, expressed by Sf9 insect cells , with C-His labeled tag.
Ebola virus VP24 Protein is an IFN antagonist, and mediates nucleocapsid assembly. VP24 inhibits IFN-activated signaling by preventing nuclear import of STAT1 via competitive binding to nuclear import receptors (karyopherins). VP24 can interact with NP and is essential for nucleocapsid formation and packaging into the virion. Ebola virus VP24 Protein (AHX24653, His) is the recombinant Virus-derived Ebola virus VP24 protein, expressed by E. coli , with N-His labeled tag. The total length of Ebola virus VP24 Protein (AHX24653, His) is 233 a.a., with molecular weight of ~28.5 KDa.
Ebola virus glycoproteins (GPs) play a key role in the virus entry process, with GP1 serving as the receptor-binding subunit and GP2 for membrane fusion.GP downregulates host cell surface molecules, disrupts adhesion and may lead to disruption of vascular integrity.Ebola virus Glycoprotein/GP1 Protein (AHX24649, HEK293, His) is the recombinant Virus-derived Ebola virus Glycoprotein/GP1 protein, expressed by HEK293 , with C-His labeled tag.
Ebola virus glycoproteins (GPs) play a key role in the virus entry process, with GP1 serving as the receptor-binding subunit and GP2 for membrane fusion. GP downregulates host cell surface molecules, disrupts adhesion and may lead to disruption of vascular integrity. Ebola virus Glycoprotein/GP1 Protein (AHX24649, sf9, His) is the recombinant Virus-derived Ebola virus Glycoprotein/GP1 protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of Ebola virus Glycoprotein/GP1 Protein (AHX24649, sf9, His) is 469 a.a., with molecular weight of ~52.3 KDa.
Ebola virus glycoproteins (GPs) play a key role in the virus entry process, with GP1 serving as the receptor-binding subunit and GP2 for membrane fusion. GP downregulates host cell surface molecules, disrupts adhesion and may lead to disruption of vascular integrity. Ebola virus Glycoprotein/GP Protein RBD (AHX24649, HEK293, Fc) is the recombinant Virus-derived Ebola virus Glycoprotein/GP protein RBD, expressed by HEK293 , with C-hFc labeled tag. The total length of Ebola virus Glycoprotein/GP Protein RBD (AHX24649, HEK293, Fc) is 308 a.a., with molecular weight of ~57.6 KDa.
Ebola virus glycoproteins (GPs) play a key role in the virus entry process, with GP1 serving as the receptor-binding subunit and GP2 for membrane fusion. GP downregulates host cell surface molecules, disrupts adhesion and may lead to disruption of vascular integrity. Ebola virus Glycoprotein/GP Protein RBD (AHX24649, HEK293, His) is the recombinant Virus-derived Ebola virus Glycoprotein/GP protein RBD, expressed by HEK293 , with C-His labeled tag. The total length of Ebola virus Glycoprotein/GP Protein RBD (AHX24649, HEK293, His) is 308 a.a., with molecular weight of ~32.3 KDa.
Ebola virus glycoproteins (GPs) play a key role in the virus entry process, with GP1 serving as the receptor-binding subunit and GP2 for membrane fusion. GP downregulates host cell surface molecules, disrupts adhesion and may lead to disruption of vascular integrity. Ebola virus Glycoprotein/GP2 Protein (AHX24649, HEK293, Fc) is the recombinant Virus-derived Ebola virus Glycoprotein/GP2 protein, expressed by HEK293 , with N-mFc labeled tag. The total length of Ebola virus Glycoprotein/GP2 Protein (AHX24649, HEK293, Fc) is 149 a.a., with molecular weight of ~43.4 KDa.
Ebola virus VP40 (matrix VP40 protein) centrally directs virus assembly and budding and has complex interactions with viral ribonucleocapsid and host ESCRT proteins (VPS4, PDCD6IP/ALIX, NEDD4, TGS101). Ebola virus VP40/Matrix VP40 Protein (AHX24648, His) is the recombinant Virus-derived Ebola virus VP40/Matrix VP40 protein, expressed by E. coli , with N-6*His labeled tag. The total length of Ebola virus VP40/Matrix VP40 Protein (AHX24648, His) is 296 a.a., with molecular weight of ~34.1 KDa.
Ebola virus glycoproteins (GPs) play a key role in the virus entry process, with GP1 serving as the receptor-binding subunit and GP2 for membrane fusion.GP downregulates host cell surface molecules, disrupts adhesion and may lead to disruption of vascular integrity.Ebola virus Glycoprotein/GP Protein (AHX24649, HEK293, His) is the recombinant Virus-derived Ebola virus Glycoprotein/GP protein, expressed by HEK293 , with C-His labeled tag.
HLA-A*0201 MAGE-A4 Complex Protein, a member of the major histocompatibility complex (MHC) class I family, is highlighted. Additionally, the Chimeric HLA-A*0201 WT-1 Complex Tetramer is recognized within the MHC class I family. HLA-A*0201 P53 WT Complex Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing human-derived HLA-A*0201 P53 WT protein, expressed by HEK293 , with C-Avi, C-His labeled tag.
Ebola virus glycoproteins (GPs) play a key role in the virus entry process, with GP1 serving as the receptor-binding subunit and GP2 for membrane fusion.GP downregulates host cell surface molecules, disrupts adhesion and may lead to disruption of vascular integrity.Ebola virus Glycoprotein/GP Protein (AIE11917, HEK293, His) is the recombinant Virus-derived Ebola virus Glycoprotein/GP protein, expressed by HEK293 , with C-His labeled tag.
HLA-A*0201 MAGE-A4 Complex Protein, a member of the major histocompatibility complex (MHC) class I family, is highlighted. Additionally, the Chimeric HLA-A*0201 WT-1 Complex Tetramer is recognized within the MHC class I family. HLA-A*0201 P53 WT Complex Protein, Human (Biotinylated, HEK293, His-Avi) is a recombinant protein dimer complex containing human-derived HLA-A*0201 P53 WT Complex protein, expressed by HEK293 , with C-Avi, C-His labeled tag. HLA-A*0201 P53 WT Complex Protein, Human (Biotinylated, HEK293, His-Avi), has molecular weight of 51-60 kDa.
HLA-A*0201 MAGE-A4 Complex Protein, a member of the major histocompatibility complex (MHC) class I family, is highlighted. Additionally, the Chimeric HLA-A*0201 WT-1 Complex Tetramer is recognized within the MHC class I family. HLA-A*0201 P53 WT Complex Tetramer Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing human-derived HLA-A*0201 P53 WT Tetramer protein, expressed by HEK293 , with C-Avi, C-His labeled tag.
HLA-A*0301 collaborates with B2M to present viral and tumor peptides, guiding CD8-positive T cell responses against infected or transformed cells. It can also present self-peptides, avoiding autoreactivity. The antigen recognition specificity involves the peptide and MHC residues, with HLA-A*0301 presenting 8 to 13 amino acid peptides, characterized by allele-specific binding motifs. Specific alleles, like A*01:01 and A*03:01, present a distinct repertoire of peptides, including viral and tumor epitopes. HLA-A*0301 KRAS WT Protein, Human (Biotinylated, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*0301 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVVGAGGVGK peptide. HLA-A*0301 KRAS WT Protein, Human (Biotinylated, HEK293, His-Avi), has molecular weight of 52-62 kDa.
HLA-A*0301 collaborates with B2M to present viral and tumor peptides that direct CD8-positive T cells to respond against infected or transformed cells. It can also present self-peptides to avoid self-reaction. HLA-A*0301 KRAS WT Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*0301 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVVGAGGVGK peptide. HLA-A*0301 KRAS WT Protein, Human (HEK293, His-Avi), has molecular weight of 52-62 kDa.
HLA-A*1101as, a pivotal MHCI molecule, presents viral and tumor-derived peptides, guiding T cell immune responses against infected or transformed cells. Collaborating with B2M, it displays a diverse peptide repertoire. Both the presented peptide and MHCI contribute to antigen recognition specificity. HLA-A*1101 typically presents 8 to 13 amino acid intracellular peptides, binding different peptides with allele-specific motifs. It plays a crucial role in controlling infections, presenting immunodominant epitopes from HIV-1, EBV, HBV, and contributing to the immune response against SARS-CoV-2. HLA-A*1101 KRAS WT Complex Protein, Human (Biotinylated, VVVGAGGVGK, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVVGAGGVGK peptide. HLA-A*1101 KRAS WT Complex Protein, Human (Biotinylated, VVVGAGGVGK, HEK293, His-Avi), has molecular weight of 53-63 kDa.
HLA-A*1101as is a key MHCI molecule that presents viral and tumor-derived peptides that direct T cell immune responses against infected or transformed cells. It collaborates with B2M to showcase a diverse peptide library. HLA-A*1101 KRAS WT Complex Protein, Human (VVVGAGGVGK, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVVGAGGVGK peptide. HLA-A*1101 KRAS WT Complex Protein, Human (VVVGAGGVGK, HEK293, His-Avi), has molecular weight of 52-62 kDa.
HLA-A*1101as is a key MHCI molecule that presents viral and tumor-derived peptides that direct T cell immune responses against infected or transformed cells. It collaborates with B2M to showcase a diverse peptide library. HLA-A*1101 KRAS WT Complex Tetramer Protein, Human (VVVGAGGVGK, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVVGAGGVGK peptide. HLA-A*1101 KRAS WT Complex Tetramer Protein, Human (VVVGAGGVGK, HEK293, His-Avi), has molecular weight of 260-265 kDa.
HLA-A*0301 collaborates with B2M to present viral and tumor peptides that direct CD8-positive T cells to respond against infected or transformed cells. It can also present self-peptides to avoid self-reaction. HLA-A*0301 KRAS WT Tetramer Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*0301 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-His, C-Avi labeled tag and VVVGAGGVGK peptide. HLA-A*0301 KRAS WT Tetramer Protein, Human (HEK293, His-Avi), has molecular weight of 260-265 kDa.
HLA-A*1101as is a key MHCI molecule that presents viral and tumor-derived peptides that direct T cell immune responses against infected or transformed cells. It collaborates with B2M to showcase a diverse peptide library. FITC-Labeled HLA-A*1101 KRAS WT Complex Protein, Human (VVVGAGGVGK, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVVGAGGVGK peptide. FITC-Labeled HLA-A*1101 KRAS WT Complex Protein, Human (VVVGAGGVGK, HEK293, His-Avi), has molecular weight of 55-60 kDa.
Amiodarone-d4 (hydrochloride) is the deuterium labeled Amiodarone hydrochloride. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ∼45 nM[1]. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts[2]. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias[1].
Tafamidis-d3 is deuterium labeled Tafamidis. Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis[1].
WTAP Antibody is a rabbit-derived non-conjugated IgG antibody, targeting WTAP, with a predicted molecular weight of 44 kDa (observed band size: 55 kDa). WTAP Antibody (YA1657) can be used for WB, IHC-P, IF experiment in human,Mouse,Rat. background.
WTAP Antibody (YA1657) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1657), targeting WTAP, with a predicted molecular weight of 44 kDa (observed band size: 55 kDa). WTAP Antibody (YA1657) can be used for WB, IHC-P, IP experiment in human background.
Wilms Tumor Protein Antibody (YA2277) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2277), targeting Wilms Tumor Protein, with a predicted molecular weight of 49 kDa (observed band size: 55 kDa). Wilms Tumor Protein Antibody (YA2277) can be used for WB, IHC-P, ICC/IF, FC experiment in human, mouse background.
PAR4 Antibody (YA2603) is a biotin-conjugated non-conjugated IgG antibody, targeting PAR4, with a predicted molecular weight of 37 kDa (observed band size: 40 kDa). PAR4 Antibody (YA2603) can be used for WB experiment in human, mouse, rat background.
DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively . DB008 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MS-II-124 is an effective and selective NLRP3 inhibitor (IC50=0.12 μM) with anti-inflammatory and immunomodulatory activities, which can be used in the research of acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) .
WT1 Human Pre-designed siRNA Set A contains three designed siRNAs for WT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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