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Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs .
Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs .
EFdA-TP tetralithium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetralithium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetralithium inhibits HIV-1 RT with multiple mechanisms .
RT-AM is a pro-agent real thiol. Real Thiol is a reversible reaction-based fluorescent probe which can quantitatively monitor the real-time glutathione dynamics in living cells.
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities .
Deoxyguanosine triphosphate (dGTP) trisodium solution (100 mM) is a nucleotide precursor in cells for DNA synthesis. Deoxyguanosine triphosphate trisodium salt is used in reverse transcription-polymerase chain reaction (RT-PCR) for DNA amplification .
1,6-Di-O-galloyl-β-D-glucose is a compound found in the fruit of Phyllanthus emblica. 1,6-Di-O-galloyl-β-D-glucose has HIV-1 reverse transcriptase (RT) inhibitory activity with an IC50 value of 270 μM. The inhibitory mechanism of 1,6-Di-O-galloyl-β-D-glucose is competitive inhibition of the template primer and non-competitive inhibition of the substrate (dTTP). 1,6-Di-O-galloyl-β-D-glucose can be used in anti-HIV research .
Tenecteplase (TNK-tPA) is a modified tissue plasminogen activator. Tenecteplase is a recombinant human tissue plasminogen activator (rt-PA) that has been bioengineered to produce mutations in three gene loci. Tenecteplase (TNK-tPA) can be used in the study of acute ischemic stroke .
EFdA-TP is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP inhibits HIV-1RT with multiple mechanisms .
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 .
Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFR L858R/T790M. EAI001 can be used for research of cancer .
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 .
EFdA-TP tetrasodium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetrasodium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetrasodium inhibits HIV-1RT with multiple mechanisms . EFdA-TP (tetrasodium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Elvucitabine is an L-nucleoside analogue. Elvucitabine is a potent nucleoside reverse transcriptase (RT) inhibitor. Elvucitabine can be used in research of viral infection .
PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFR L858R-T790M (NCI-H1975 cells), EGFR L858R (NCI-H3255 cells), and EGFR L858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM .
PROTAC EGFR degrader 16 (Compound 98) a selective EGFR PROTAC degrader with DC50 values of < 50 nM in NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R) and NCI-H1976 + CS (EGFR L858R-T970M-L797S). PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer (Pink: EGFR ligand (HY-178313); Blue: CRBN ligand (HY-W1128702); Black: Linker; EGFR ligand + Linker (HY-178311)) .
EGFR-IN-126 (compound 9d) is a potent inhibitor of EGFR L858R/T790M/C797S, with the IC50 value of 0.005 μM. EGFR-IN-126 shows antitumor effects in vivo and in vitro .
Roseltide rT1 is a neutrophil elastase inhibitor (IC50=0.47 μM) rich in cysteine and one of the Roseltide (rT1-rT8) family members. Roseltide rT1 improves cAMP accumulation stimulated by neutrophil elastase in vitro, showing potential for inhibiting related diseases .
RT-NH2 is a RealThiol prototype without the carboxylic acid groups. RT-NH2 is fairly hydrophobic and cannot distribute in the nucleus, which is a hallmark of protein binding for fluorescent probe.
Tivirapine (R86183) is a nonnucleoside HIV-1 RT inhibitor against HIV-1-induced cytopathic effects with an EC50 value of 4 nM. Tivirapine inhibits the Yl8lC mutant of HIV-1 RT .
Anti-Mouse/Rat MHC Class II (I-Ek/RT1-D) Antibody (14-4-4S) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to mouse/rat MHC Class II. Anti-Mouse/Rat MHC Class II (I-Ek/RT1-D) Antibody (14-4-4S) reacts with mouse MHC Class II alloantigen I-Ek and the rat MHC class II alloantigen RT1D. Anti-Mouse/Rat MHC Class II (I-Ek/RT1-D) Antibody (14-4-4S) blocks antigen presentation. Anti-Mouse/Rat MHC Class II (I-Ek/RT1-D) Antibody (14-4-4S) can be used for the research of immunology and cancer .
EFdA-TP tetraammonium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetraammonium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetraammonium inhibits HIV-1RT with multiple mechanisms . EFdA-TP (tetraammonium) 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-IN-84 (Compound 9) is a potent HIV-1 non-nucleoside reverse transcriptase (HIV-1 RT) inhibitor (IC50=33.89 μM, EC50=540 nM). HIV-1-IN-84 is promising for research of HIV infections .
Mer-NF5003E is a non-nucleoside reverse transcriptase inhibitor targeting HIV-1 reverse transcriptase (RT) (EC50=50 μM). Mer-NF5003E exhibits inhibitory activity against wild-type HIV-1 and multiple NNRTI-resistant strains (e.g., K103N, Y181C). Mer-NF5003E is promising for research of HIV infections .
Fozivudine tidoxil (BM-211290) is an orally active thioether lipid-zidovudine (ZDV) conjugate with anti-HIV activity. Fozivudine tidoxil, a member of the NRTI family of agent, is incorporated into the newly synthesized strand of DNA during intracellular viral replication and irreversibly binds viral RT which disrupts viral reverse-transcription . Fozivudine tidoxil is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Rp-TTPαS (tetrasodium) is the Rp-isomer of TTPαS (tetrasodium). Rp-TTPαS (tetrasodium) incorporate with HIV-1 reverse transcriptase (HIV-1 RT) with HIV-1 RT with large phosphorothioate elemental effects .
NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC50 of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics .
Sp-TTPαS is a competitivesterile alpha motif and HD domain containing protein 1 (SAMHD1) hydrolysis inhibitor. Sp-TTPαS competitively inhibits SAMHD1 triphosphohydrolase activity with a Ki value of 46 µM .
Trovirdine hydrochloride, a phenethylthiazolylthiourea (PETT) derivative, is an HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI). A novel computer model of the RT/NNI binding pocket revealed spatial gaps around Trovirdine hydrochloride's pyridyl ring. Docking studies suggested that replacing this planar ring with a nonplanar piperidinyl or piperazinyl ring could better occupy the binding pocket, enhancing anti-HIV activity. Synthesized heterocyclic compounds based on this modification demonstrated greater potency than Trovirdine hydrochloride, effectively inhibiting HIV replication at nanomolar concentrations without cytotoxicity in infected peripheral blood mononuclear cells .
EGFR-IN-69 (compound 17g) is a potent EGFR inhibitor, with IC50 values of 4.3, 6.6 and 25.6 nM against EGFR L858R/T790M/C797S, EGFR L858R/T790M, and EGFR 19del/T790M/C797S, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research .
Pseudoginsenoside RT5 (Standard) is the analytical standard of Pseudoginsenoside RT5. This product is intended for research and analytical applications. Pseudoginsenoside RT5 is isolated from Panax quinquefolium .
RT2 is a tryptophan-rich cationic amphipathic antibacterial peptide, with main targets including lipopolysaccharide (LPS) on the bacterial surface and intracellular DNA. RT2 binds to bacterial surface LPS, and interacts with cytoplasmic membrane phospholipids, enabling it to rapidly penetrate the bacterial cell membrane and enter the cell, and then bind to components such as DNA in the cytoplasmic membrane, thereby exerting antibacterial effects. RT2 is promising for research of acute and chronic infections caused by planktonic bacteria .
Moloney murine leukemia virus RT is a monomeric reverse transcriptase from Moloney murine leukemia virus (MMLV). Moloney murine leukemia virus RT is a replicative polymerase that play an essential role in the life cycle of the retrovirus .
Pol (476-484), HIV-1 RT Epitope is a biological active peptide. (This is a reverse transcriptase (RT) epitope (Pol residues 476-484). Within HIV-1 RT the peptide appears to be the dominant HLA A*0201-restricted epitope. Was used to investigate possible mechanisms behind HIV-1 escape from CTL. IV9 is the actual epitope processed and presented in HIV-1-infected cell lines.)
HIV-1 inhibitor-30 (compound 10i) is a potent HIV-1 inhibitor with an EC50 value of 40 nM and an IC50 value of 80 nM for HIV-1 RT DNA polymerase. HIV-1 inhibitor-30 has highly antiretroviral activity against seven non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains (RT-K103N; RT-Y181C; RT-K103N,Y181C; RT-L100I,K103N; RT-Y188L; RT-K103N,G190A; RT-K103N,V108I) with IC50s of 0.04~1.42 μM. HIV-1 inhibitor-30 can be used for researching AIDS .
BM 21.1298 is a selective and high specific nonnucleoside immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) inhibitor with antiviral activity .
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC50s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively .
4-Aminodiphenylamine sulfate (Variamine Blue RT sulfate) is a multifunctional dye. Dyes are important tools in biological experiments. They can help researchers observe and analyze cell structures, track biomolecules, evaluate cell functions, distinguish cell types, detect biomolecules, study tissue pathology and monitor microorganisms. Their applications range from basic scientific research to clinical A wide range of diagnostics. Dyes are also widely used in traditional fields such as textile dyeing, as well as in emerging fields such as functional textile processing, food pigments and dye-sensitized solar cells.
TNK-6123 is a potent Emivirine (HY-15353) analogue with improved activity against drug-resistant HIV mutants. TNK-6123 improves activity against Lys103Asn mutant RT .
Hydroxyisoquinoline-1,3(2H,4H)-dione (compound 6a) is a HIV-1 integrase (IN) and HIV-1 reverse transcriptase (RT) ribonuclease H (RNase H) inhibitor with an IC50 value of 6.32, 5.9 µM, respectively .
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) .
Delavirdine (mesylate) (Standard) is the analytical standard of Delavirdine (mesylate). This product is intended for research and analytical applications. Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26?μM) over DNA polymerase?α?(IC50=440 μM) and polymerase?δ (IC50>550?μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs .
Delavirdine (Standard) is the analytical standard of Delavirdine. This product is intended for research and analytical applications. Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26?μM) over DNA polymerase?α?(IC50=440 μM) and polymerase?δ (IC50>550?μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs .
S-2720 is a potent inhibitor of both immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) and HIV-1 replication. The binding sites of S-2720 and the nonnucleoside compounds overlap. The small pocket in the p66 subunit-BI-RG-587 (HY-10570) complex is most likely the target of S-2720. S-2720 is a quinoxaline derivative, which is promising for research of HIV-1 infection .
POMT1 Human Pre-designed siRNA Set A contains three designed siRNAs for POMT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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 .
HIV-1 inhibitor-42 (compound 5b) is a potent HIV-1 inhibitor, with an IC50 of 0.06 μM. HIV-1 inhibitor-42 inhibits HIV-1 RT RNA-dependent DNA polymerase and DNA-dependent DNA polymerase, with IC50 values of 0.518 and 0.072 μM .
HIV-1 inhibitor-13 (compound 16c) is a orally active and potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), with IC50 of 0.14 μM (HIV-1 RT). HIV-1 inhibitor-13 shows activity against a panel of HIV-1 resistant strains, with EC50 values of 2.85-18.0 nM .
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
GS-9148 is a ribose-modified HIV-1 nucleotide reverse transcriptase (RT) inhibitor with an EC50 value of 10.6 µM. GS-9148 shows antiretroviral activity for K65R, L74V, or M184V RT mutation .
Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively .
Antitumor agent-99 (compound 7) is an anticancer agent targeting FRα/β and PCFT. Antitumor agent-99 inhibits R2/PCFT4 (PCFT), RT16(FRα), and D4(FRβ) cells with IC50s of 51.46 nM, 2.53 nM, and 2.98 nM, respectively .
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 .
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 .
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)
EGFR-IN-27 is a potent EGFR inhibitor with IC50s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511) .
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) .
BILR 355 is a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI). BILR 355 is highly specific toward HIV-1 reverse transcriptase (RT). BILR 355 can be used for HIV infections research .
EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a EGFR inhibitor. The IC50 values for EGFR L858R/T790M/C797S and Ba/F3-EGFR L858R/T790M/C797S are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC) .
EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC50 value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research .
EGFR-IN-133 (Compound 24) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. EGFR-IN-133 exhibits good pharmacokinetics characteristics with high oral exposure .
EGFR-IN-132 (Compound 23) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 1.6, 0.025, 0.019, 0.022, and 0.029 nM. EGFR-IN-132 exhibits good pharmacokinetics characteristics with high oral exposure .
EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC50s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research[1].
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 .
HIV RT-IN-2 is a HIV reverse transcriptase inhibitor with an IC50 value of 1.2 μM for HIV-1RT RNA-dependent DNA polymerase. HIV RT-IN-2 potently inhibits all three modes of HIV-1 RT-associated RNase H activity (internal, 3'-DNA directed, 5'-RNA directed cleavage) and inhibits HIV-1 replication. HIV RT-IN-2 can be used for the research of HIV-1 infection .
Pseudoginsenoside RT4 is an orally active tetracyclic triterpenoid. Pseudoginsenoside RT4 can be isolated from Panax pseudoginseng subsp. Himalaicus. Pseudoginsenoside RT4 reduces the levels of pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β), boosts the levels of IL-10. Pseudoginsenoside RT4 modulates the composition of gut microbiota. Pseudoginsenoside RT4 shows anti-inflammatory effects. Pseudoginsenoside RT4 can be used in the study of ulcerative colitis .
HIV RT-IN-1 is an inhibitor of HIV integrase and HIV reverse transcriptase-associated ribonuclease H. HIV RT-IN-1 is applicable to research related to HIV-1 infection .
RT-NH2 (Standard) is the analytical standard of RT-NH2 (HY-103684). This product is intended for research and analytical applications. RT-NH2 is a RealThiol prototype without the carboxylic acid groups. RT-NH2 is fairly hydrophobic and cannot distribute in the nucleus, which is a hallmark of protein binding for fluorescent probe.
Vintoperol (RGH 2981; RT-3003) is a potent and orally active antithrombotic agent. Vintoperol interferes with platelet aggregation and has antithrombotic effects, protecting mice from retrograde and anterograde amnesia induced by traumatic brain injury .
Soulattrolide is a non-nucleoside HIV-1 reverse transcriptase (RT) inhibitor with IC50 values of 0.34 µM for HIV-1 RT, 69.5 µM for E. coliRNase H, and >495 µM for human DNA polymerase β, and can be found in Calophyllum teysmannii latex. Soulattrolide can be used for the research of HIV-1 infection, pain, inflammation, and Mycobacterium tuberculosis infection .
U 88204 is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 of 0.25 μM. U 88204 blocks HIV-1 replication in infected cells. U 88204 can be used for the research on HIV-infection and of acquired immunodeficiency syndrome (AIDs) .
NNRT-IN-16, Rilpivirin (HY-10574) analogue, is a non-nucleoside reverse transcriptase inhibitor (NNRTI). NNRT-IN-16 inhibits recombinant WT HIV-1RT with an IC50 of 0.07 μM. NNRT-IN-16 exerts antiviral activity against wild-type and drug-resistant HIV-1 mutants, shows attenuated CYP isoenzyme and hERG inhibition, reduced cytotoxicity, and improved metabolic stability in human liver microsomes. NNRT-IN-16 can be used for the research of HIV-1 infection .
Cytosolic 5'-nucleotidase II, Huamn (EC 3.1.3.5) is a pure and active protein cloned by RT-PCR amplification of mRNA extracted from human hepatoma cells and expressed in E.coli.
EGFR-IN-208 is an allosteric mutant EGFR L858R/T790M and EGFR L858R/T790M/C797S inhibitor, with IC50 values of 3.06 μM and 1.08 μM, respectively. EGFR-IN-208 binds to the allosteric site of EGFR and inhibits EGFR phosphorylation. EGFR-IN-208 induces apoptosis and exhibits antiproliferative effects in cancer cells. EGFR-IN-208 can be used in research related to non-small cell lung cancer .
Gly-PEG3-BA is an EML4-ALKPROTAC degrader. Gly-PEG3-BA effectively reduces EML4-ALK with a DC50 value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC50 of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC50s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research .
NNRT-IN-15 (Compound 16a) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor. NNRT-IN-15 shows an EC50 of 3 nM for WT HIV-1 and inhibits seven mutant strains (L100I, K103N, Y181C, etc.) (EC50 = 8.2-43.4 nM). NNRT-IN-15 has low cytotoxicity against MT-4 cells (CC50 = 196.46 μM). NNRT-IN-15 also inhibit WTHIV-1RT and hERG with IC50 values of 0.7599 μM and 27.455 μM. NNRT-IN-15 can be used for research of HIV-1 infection .
FGFR-IN-24 (Compound 8r) is a FGFR inhibitor. FGFR-IN-24 potently inhibits FGFR1/2/3 with IC50 values of 10.0, 6.9, and 30.2 nM, respectively. FGFR-IN-24 exhibits superior inhibitory activity toward FGFR1 V561M, FGFR2 V564F, and FGFR2 N549K mutations with IC50 values of 6.8, 0.7, and 0.8 nM, respectively. FGFR-IN-24 induces Apoptosis. FGFR-IN-24 efficiently suppresses the phosphorylation of FGFR2 and its downstream signaling mediators (AKT and MAPK). FGFR-IN-24 demonstrates favorable antitumor efficacy in an RT112/84 bladder cancer xenograft model .
EGFR-IN-22 is a potent EGFR inhibitor with IC50s of 4.91 nM and 0.54 nM for wild type EGFR and EGFR L858R/T790M/C797S, respectively (CN112538072A, compound 243) .
HIV-IN-9 (Compound 2b) is a HIV inhibitor (IC50: 6.65 μg/mL), and has high binding affinity with HIV-RT. HIV-IN-9 also inhibits CYP3A4, CYP1A2, CYP2C1, and CYP2D6 .
Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy .
dUTP sodium is the salt form of dUTP. dUTP is a metabolic intermediate in both procaryotes and eucaryotes. dUTP can be used in PCR and RT-PCR to replace dTTP, resulting in the uracil-containing PCR products suitable for most standard applications. dUTP is found to inhibit the enzyme - Cytidine Aminohydrolase from sheep liver .
EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity .
Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
L-697639 is an inhibitor for HIV-1 reverse transcriptase (HIV-1 RT) with IC50 of 20-400 nM (in a template-primer-dependent manner). L-697639 exhibits antiviral activity, that inhibits 95% HIV-1 infection at concentrations of 12-200 nM in human T lymphocyte cultures .
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 .
ZSH-2117 is a covalent and selective EGFRPROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFR L858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFR L858R/T790M/C797S xenograft mice model . Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR L858R/T790M/C797S cells at the concentration of 0.8 μM .
JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
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 .
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
EGFR ligand-2 (compound C4), a covalent EGFR ligand, is a EGFR mutant inhibitor with IC50s of 21 nM and 48 nM for EGFR L858R and EGFR L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
Osimertinib (dimesylate) (Standard) is the analytical standard of Osimertinib (dimesylate). This product is intended for research and analytical applications. Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
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) .
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 .
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively .
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
JLJ648 is a Gag-Pol dimerizer with antiviral activity. JLJ648 can inhibit HIV replication and induce infected cell pyroptosis. JLJ648 can be used for the research of infection, such as HIV (human immunodeficiency virus) .
HIV-1-IN-92 is a non-nucleoside inhibitor of HIV-1 reverse transcriptase with an IC50 of 0.11 μM against HIV-1 reverse transcriptase. HIV-1-IN-92 exhibits activity against both wild-type HIV-1 IIIB and mutant HIV-1 strains. HIV-1-IN-92 can be used in research related to acquired immunodeficiency syndrome (AIDS) .
Talviraline is a non-nucleoside reverse transcriptase (NNRT) inhibitor that is primarily used to inhibit the replication of human immunodeficiency virus type 1 (HIV-1). Talviraline inhibits the viral replication process by binding to a specific site of HIV-1 reverse transcriptase (RT). Talviraline can be used to study the potential countermeasures and safety of HIV-1 infection .
EGFR-IN-47 is a potent and orally active EGFR L858R/T790M/C797S inhibitor with an IC50 of 0.01 μM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC .
AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFR L858R/T790M, EGFR L858R, EGFR L861Q, EGFR and ErbB4, respectively.
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
CI-39 is an antiviral natural product. CI-39 is an NNRTI (non-nucleoside reverse transcriptase inhibit) antiviral agent with an EC50 of 3.40 μM and an CC50 of >30 μM for wild type HIV-1. CI-39 inhibits HIV-1 RT DNA polymerase and ribonuclease H activitiessup .
Rociletinib (Standard) is the analytical standard of Rociletinib. This product is intended for research and analytical applications. Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of EGFR, and thereby inhibits the downstream ERK and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR L858R/T790M mutation, and fungal infections .
EGFR-IN-197 is an EGFR inhibitor with IC50 values of 19.5 nM and 12.0 nM against EGFR L858R/T790M and EGFR L858R/T790M/C797S, respectively. EGFR-IN-197 arrests the cell cycle of NCI-H1975 cells at the G2/M phase, while inhibiting their proliferation, colony formation and migration; it also inhibits mitochondrial translocation and upregulates mitochondrial H2S levels. EGFR-IN-197 disrupts anti-apoptotic signaling pathways by regulating apoptosis-related proteins; it induces DNA damage and activates pro-apoptotic pathways to trigger apoptosis. EGFR-IN-197 can be used in studies related to non-small cell lung cancer (NSCLC) .
EGFR-IN-177 is a potent EGFR inhibitor with IC50s of 0.32, 1.04, 0.65, 0.67, 0.48, 0.55 and 0.38 nM against EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S, EGFR D746-750, EGFR D746-750/C797S, EGFR D770_N77linsNPG, and EGFR WT. EGFR-IN-177 inhibits lung cancer proliferation and EGFR phosphorylation. EGFR-IN-177 can be used for the study of cancers such as non-small cell lung cancer .
AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively .
EGFR-IN-179 (Compound 8d) is an EGFR inhibitor (IC50: 0.068 μM for EGFR L858R/T790M/C797S; 2.56 μM for EGFR-WT-TK). EGFR-IN-179 has anticancer activity against non-small cell lung cancer .
dUTP trisodium (2´-Deoxyuridine, 5´-Triphosphate) is the salt form of dUTP. dUTP is a metabolic intermediate in both procaryotes and eucaryotes. dUTP can be used in PCR and RT-PCR to replace dTTP, resulting in the uracil-containing PCR products suitable for most standard applications. dUTP is found to inhibit the enzyme - Cytidine Aminohydrolase from sheep liver .
HIV-1 inhibitor-26 (compound 9a) is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 value of 1.4 μM. HIV-1 inhibitor-26 has low cytotoxicity with a CC50 of 1486 μM in PBMCs. HIV-1 inhibitor-26 can be used for researching AIDS .
JS04 is a EGFR L858R/T790M kinase inhibitor. JS04 activates both endogenous and exogenous apoptosis (apoptosis) pathways and induces G2/M phase arrest of the cell cycle. JS04 is applicable to the research of drug-resistant non-small cell lung cancer .
AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
HIV-IN-5 (compound 5r) is a potent HIV-1 inhibitor, with an IC50 of 0.16 μM. HIV-IN-5 shows inhibition of HIV DNA-dependent DNA polymerization activity, with an IC50 of 2.18 μM. HIV-IN-5 can bind to NNIBP (NNRTIs (non-nucleoside reverse transcriptase inhibitors) binding pocket) .
Anti-Mouse CD83 Antibody (Michel-17) is a rat-derived IgG1 κ type antibody inhibitor, targeting to mouse CD83. Anti-Mouse CD83 Antibody (Michel-17) can block CD83 and inhibit T cells proliferation. Anti-Mouse CD83 Antibody (Michel-17) can be used for the researches of cancer and immunology, such as solid tumor .
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750 and EGFR E746_A750/T790M, respectively.
Rociletinib hydrobromide (Standard) is the analytical standard of Rociletinib hydrobromide. This product is intended for research and analytical applications. Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
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 .
EAI001 (Standard) is the analytical standard of EAI001 (HY-100214). This product is intended for research and analytical applications. EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer .
EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of L858R/T790M/C797S mutant EGFR kinases, with an IC50 of 0.87 nM. EGFR-IN-161 can induce apoptosis process, G1-phase arrestation, and migration inhibition in tumor cells .
PROTAC GPX4 degrader-4 is a GPX4 PROTAC degrader (DC50: 5.32 nM). PROTAC GPX4 degrader-4 inhibits the activity of RT4, T24, and J82 cancer cells (IC50 values are 0.09, 2.97, and 7.58 μM, respectively). PROTAC GPX4 degrader-4 increases lipid ROS levels and induces ferroptosis in T24 and RT4 cells. PROTAC GPX4 degrader-4 has antitumor activity in T24 tumor-bearing BALB/c nude mouse model. PROTAC GPX4 degrader-4 can be used for bladder cancer research. (Pink: target protein ligand (HY-N0193); blue: E3 ligase ligand (HY-1035960); black: linker (HY-W013907); E3 ligase ligand + linker (HY-174087)) .
DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer .
EGFR-IN-87 (Compound Example 2) 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 .
EGFR-IN-164 (Compound 4) is a selective and covalent allosteric EGFR inhibitor. EGFR-IN-164 significantly inhibits the activity of EGFR L858R/T790M/C797S kinase (IC50: 48.1 nM) and proliferation of of EGFR-mutant cells. EGFR-IN-164 can be used for drug resistance of cancer research .
EGFR-IN-87 (Compound Example 2) hydrochloride is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 hydrochloride 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 hydrochloride can be used for cancer diseases research .
WZ3146 is a mutant selective EGFR inhibitor with IC50s of
2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively.
EGFR-IN-95 (compound 5j) is an 2,4-diaminonicotinamide derivative. EGFR-IN-95 has potent inhibitory activity against EGFR del19/T790M/C797S and L858R/T790M/C797S .
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .
HIV-1 invistor-50 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that targets HIV-1 reverse transcriptase (RT) (IC50=50 nM). HIV-1 inhibitor-50 shows significant antiviral activity, with EC50s of 2.22-53.3nM against HIV-1 IIIB and its mutant strains .
EGFR-IN-98 (Compound 4c) is a EGFR inhibitor. The IC50 values of L858R/T790M/C797S and Del19/T790M/C797S are 0.277 μM and 0.089 μM, respectively. EGFR-IN 98 can be used in the study of tumors .
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK .
HIV-1 inhibitor-53 is a dual HIV-1 protease and reverse transcriptase inhibitor. HIV-1 inhibitor-53 inhibits HIV-1 protease (PR) and reverse transcriptase (RT) activity with IC50 values of 1.93 nM and 2.35 μM, respectively. HIV-1 inhibitor-53 can be used for the research of acquired immune deficiency syndrome (AIDS) .
EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC) .
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 .
Osimertinib dimer is a dimer of Osimertinib (HY-15772). Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Osimertinib (mesylate) (Standard) is the analytical standard of Osimertinib (mesylate). This product is intended for research and analytical applications. Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
EGFR-IN-24 is a selective EGFR triple mutant inhibitor with >300 nM IC50 against human EGFRdel19/T790M/C797S, EGFRL858R/T790M/C797S, and EGFRWT. EGFR-IN-24 can be used for the research of non-small cell lung cancer .
HIV-1 inhibitor-39 (compound 3c) is a potent HIV-1 inhibitor with an EC50 of >112.88 µM. HIV-1 inhibitor-39 shows anti-RT (HIV-1 reverse transcriptase) activities with an IC50 of 15.75 µM. HIV-1 inhibitor-39 shows cytotoxicity for MT-4 cells with an CC50 of 112.9 µM .
Sennoside A is an anthraquinone glycoside found in senna (Cassia angustifolia). Sennoside A is an HIV-1 inhibitor (IC50=3.8 μM) that inhibits HIV-1 replication. Sennoside A also inhibits HIV-1 reverse transcriptase (RT)-related DNA polymerase (RDDP) and ribonuclease H (Ribonuclease H) with IC50s of 1.9 μM and 5.3 μM, respectively .
EGFR-IN-104 (Compound A23) is an effective inhibitor of EGFR, with IC50 values of 0.33 μM and 0.133 μM against EGFR L858R/T790M and EGFR Del19/T790M/C797S, respectively. EGFR-IN-104 exhibits anticancer activity both in vitro and in vivo .
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 .
Icotinib (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) 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-IN-180 (Compound L15) is an EGFR inhibitor. EGFR-IN-180 shows inhibitory activity against EFGR and EGFR harboring the L858R/T790M/C797S triple drug-resistant mutation, with IC50 values of 80.96 nM and 16.43 nM, reapectively. EGFR-IN-180 can be used for the study of non-small cell lung cancer (NSCLC) .
EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer .
EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFR L858R/T790M and EGFR Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .
HIV-1 inhibitor-57 (Compound 12g) is a HIV inhibitor. HIV-1 inhibitor-57 is active against wild-type and five prevalent NNRTI-resistant HIV-1 strains with EC50 values ranging from 0.024 to 0.0010 μM. HIV-1 inhibitor-57 forms additional interactions with residues around the binding site in HIV-1 RT .
EAI045 (Standard) is the analytical standard of EAI045 (HY-100213). This product is intended for research and analytical applications. EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.
JBJ-07-149 is an inhibitor for EGFRL858R/T790M with an IC50 of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC50 of 4.9 μM and 0.148 μM, without and with presence of Cetuximab (HY-P9905). JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163 (HY-139997) .
Icotinib (Hydrochloride) (Standard) is the analytical standard of Icotinib (Hydrochloride). This product is intended for research and analytical applications. Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity . 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFR del19 and EGFR L858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy .
NNRT-IN-6 (Compound 13a) is the non-nucleoside reverse transcriptase inhibitor (NNRT) for HIV-1 reverse transcriptase (HIV-1 RT) with IC50 of 0.41 μM. NNRT-IN-6 inhibits HIV-1 wildtype and mutant strains L100I, K103N, Y181C, Y188L, E138K, F227L/V106A and RES056 with EC50 of 6.2-250 nM .
EGFR-IN-175 is an orally active and selective EGFR L858R/T790M/C797S inhibitor with an IC50 of 18.94 nM. EGFR-IN-175 can induce cell apoptosis and cause G1 phase arrest. EGFR-IN-175 can downregulate p-EGFR, p-AKT, and p-ERK expression. EGFR-IN-175 can be used for the research of cancer, such as lung cancer .
EGFR-IN-451 is an EGFR inhibitor with an IC50 value of 0.02 nM. EGFR-IN-451 also inhibits mutant EGFRL858R, EGFRT790M, and EGFRL858R/T790Mwith IC50 values of 0.26-34 nM. EGFR-IN-451 inhibits AKT and ERK activation and inhibits proliferation of EGFR-mutant cancer cells. EGFR-IN-451 can be used for the research of EGFR-driven cancer .
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
EGFR-IN-213 is a selective inhibitor of EGFRL858R/T790M/C797S with a human IC50 of 0.48 nM. EGFR-IN-213 acts as an antiproliferative agent, inducing apoptosis and cell cycle arrest, and inhibiting colony formation, cell migration, and tube formation. EGFR-IN-213 can be used for the research of non-small cell lung cancer, chronic myeloid leukemia, gastric cancer, prostate cancer .
EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with Ki of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC50 of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model .
anti-HIV agent 1 (compound 10i) is a potent antiviral agent with anti-HIV activity (IC50 = 10.6 nM). anti-HIV agent 1 exhibits moderate to no inhibitory activity against RT mutant strains, but maintains their activity against wild-type viruses. anti-HIV agent 1 strongly shows dual inhibition of the viral attachment and reverse transcriptase phases of the viral life cycle. anti-HIV agent 1 can be used for HIV infection research .
EGFR/PI3Kα-IN-1 (compound 30k) is a dual EGFR/PI3Kα inhibitor with IC50 values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα), respectively. EGFR/PI3Kα-IN-1 can inhibit tumor cell proliferation and has anticancer activity .
NNRT-IN-12 (compound 19) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor with an IC50 value of 0.107 μM for WT HIV-1 RT. NNRT-IN-12 shows anti-HIV-1 activity with EC50 value of 14.1, 5.03, 7.64, 27.1 nM for L100I, K103N, Y181C, Y188L mutant HIV-1 strains, respectively. NNRT-IN-12 shows cytotoxicity .
2'-Deoxyadenosine-5'-triphosphate trisodium,100 mM Solution,PCR Grade (dATP trisodium,100 mM Solution,PCR Grade) is one of the raw materials used by DNA polymerase to synthesize long DNA strands during DNA replication. 2'-Deoxyadenosine-5'-triphosphate trisodium,100 mM Solution,PCR Grade is used in reverse transcription polymerase chain reaction (RT-PCR) for DNA amplification. This product is supplied in the form of an aqueous solution .
Icotinib (Standard) is the analytical standard of Icotinib. This product is intended for research and analytical applications. Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib 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-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 .
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
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) 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 .
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
AV-412 free base (Standard) is the analytical standard of AV-412 free base (HY-10346A). This product is intended for research and analytical applications. AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
LSD1/EGFR-IN-1 (compound L-1) is a potent inhibitor of LSD1, EGFR T790M/L858R and EGFR L858R/T790M/C797S, with IC50s of 6.24 and 2.06 and 5.01 μM, respectively. LSD1/EGFR-IN-1 plays an important role in cancer research .
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 .
Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively . Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection .
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. 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 EGFRwt, EGFRL858R, EGFRL858R/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 .
EGFR-IN-152 (compound D4) is a potent EGFR tyrosine kinase inhibitor, exhibiting potent EGFR L858R/T790M/C797S inhibition activity (IC50 = 40 nM). EGFR-IN-152 induces G0/G1 phase cell cycle arrest and apoptosis, thereby inhibiting colony formation and cell proliferation of non-small cell lung cancer (NSCLC) cells. EGFR-IN-152 can be used for NSCLC research .
Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .
Lys-PEG3-BA is an EML4-ALK/EGFRPROTAC degrader with DC50 values of 1.32 and 19.66 μM for H3122 (EML4-ALK) and H1975 (EGFR-L858R/T790M) cells, respectively. Lys-PEG3-BA hinders proliferation via rewiring the ubiquitin- proteasome system in vitro. Lys-PEG3-BA can be used for non-small cell lung cancer research .
EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases .
Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. 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 EGFRwt, EGFRL858R, EGFRL858R/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 .
EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .
BI-8128 is a potent EGFR inhibitor, with IC50 values of 12, 6.7, 22, 10, and 3 nM against wild-type, T790M, C797S, T790M/C797S, and L858R/T790M/C797S mutant EGFR, respectively. BI-8128 significantly inhibits the proliferation of Ba/F3 and PC-9 drug-resistant mutant cells. BI-8128 is applicable for the research of non-small cell lung cancer .
PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFR L858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)) .
Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=＜1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity .
EGFR T790M/L858R-IN-3 (compound B1) is a EGFR L858R/T790M inhibitor with IC50 value of 13?nM. EGFR T790M/L858R-IN-3 shows anti-tumour activity in H1975 cells with an IC50 value of 0.087 μΜ. EGFR T790M/L858R-IN-3 inhibits cell migration in A549 cells and induces apoptosis in H1975 cells .
(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 .
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 .
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 .
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFR L858R/T790M and EGFR WT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma .
FGFR-IN-23 (Compound 9p) is a covalent pan FGFR inhibitor with IC50s of 14, 4.2, 5 and 220 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-23 also has potent inhibitory activity against gatekeeper mutants, such as FGFR1 V561M and FGFR3 V555M. FGFR-IN-23 suppresses the activation of FGFR-mediated signaling and induces apoptosis. FGFR-IN-23 shows significant antitumor efficacy in RT112 xenograft mouse models. FGFR-IN-23 can be used for cancers and its drug resistance research .
EGFR-IN-160 (Compound R12) is an EGFR inhibitor (IC50 values are 1.62, 0.49 and 0.98 μM for EGFR WT, EGFR T790M and EGFR L858R/T790M/C797S, respectively). EGFR-IN-160 induces G2/M and S phase arrest and apoptosis in NCI-H522 cells, and has anticancer activity. EGFR-IN-160 has antioxidant effects against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM) .
IW927 is a photochemically enhanced TNF-α-TNFR1 interaction inhibitor that blocks the binding of TNF-α to TNFRc1 with an IC50 value of 50 nM. IW927 binds reversibly to the TNFRc1 with weak affinity (Kd = 40-100 μM), covalently modifies the receptor via a photochemical reaction, and does not bind the related cytokine receptors TNFRc2 or CD40. IW927 disrupts TNFα-induced IκB phosphorylation with an IC50 value of 600 nM. IW927 can be used to develop light-independent inhibitors .
EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
HJM-561 is a selective and effective orally active EGFRPROTAC degrader. HJM-561 is able to overcome the triple EGFR mutations that are resistant to Osimertinib (HY-15772). HJM-561 exhibits potent degradation of EGFR Del19/T790M/C797S (DC50: 9.2 nM) and L858R/T790M/C797S (DC50: 5.8 nM), and has anti-tumor activity (pink: EGFR ligand (HY-12857); blue: CRBN ligand (HY-A0003); black: linker) .
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-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) .
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 .
Pro-PEG3-BA is an EML4-ALK/EGFRPROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC 50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research .
EGFR-IN-77 (Compound 4a) is a selective EGFR T790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFRT790M/L858R, 0.477 μM against EGFRL858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFRT790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFRL858R/T790M double-mutant non-small cell lung cancer .
Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 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-IN-93 is a HIV-1 RNase H inhibitor with an IC50 of 6.09 μM. HIV-1-IN-93 shows low cytotoxicity and can be used in studies related to HIV-1 infection .
PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFR C797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFR WT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)) .
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC50 < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .
EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR 19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .
EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC) .
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
RT-NH2 is a RealThiol prototype without the carboxylic acid groups. RT-NH2 is fairly hydrophobic and cannot distribute in the nucleus, which is a hallmark of protein binding for fluorescent probe.
4-Aminodiphenylamine sulfate (Variamine Blue RT sulfate) is a multifunctional dye. Dyes are important tools in biological experiments. They can help researchers observe and analyze cell structures, track biomolecules, evaluate cell functions, distinguish cell types, detect biomolecules, study tissue pathology and monitor microorganisms. Their applications range from basic scientific research to clinical A wide range of diagnostics. Dyes are also widely used in traditional fields such as textile dyeing, as well as in emerging fields such as functional textile processing, food pigments and dye-sensitized solar cells.
RT-NH2 (Standard) is the analytical standard of RT-NH2 (HY-103684). This product is intended for research and analytical applications. RT-NH2 is a RealThiol prototype without the carboxylic acid groups. RT-NH2 is fairly hydrophobic and cannot distribute in the nucleus, which is a hallmark of protein binding for fluorescent probe.
Deoxyguanosine triphosphate (dGTP) trisodium solution (100 mM) is a nucleotide precursor in cells for DNA synthesis. Deoxyguanosine triphosphate trisodium salt is used in reverse transcription-polymerase chain reaction (RT-PCR) for DNA amplification .
2'-Deoxyadenosine-5'-triphosphate trisodium,100 mM Solution,PCR Grade (dATP trisodium,100 mM Solution,PCR Grade) is one of the raw materials used by DNA polymerase to synthesize long DNA strands during DNA replication. 2'-Deoxyadenosine-5'-triphosphate trisodium,100 mM Solution,PCR Grade is used in reverse transcription polymerase chain reaction (RT-PCR) for DNA amplification. This product is supplied in the form of an aqueous solution .
Roseltide rT1 is a neutrophil elastase inhibitor (IC50=0.47 μM) rich in cysteine and one of the Roseltide (rT1-rT8) family members. Roseltide rT1 improves cAMP accumulation stimulated by neutrophil elastase in vitro, showing potential for inhibiting related diseases .
RT2 is a tryptophan-rich cationic amphipathic antibacterial peptide, with main targets including lipopolysaccharide (LPS) on the bacterial surface and intracellular DNA. RT2 binds to bacterial surface LPS, and interacts with cytoplasmic membrane phospholipids, enabling it to rapidly penetrate the bacterial cell membrane and enter the cell, and then bind to components such as DNA in the cytoplasmic membrane, thereby exerting antibacterial effects. RT2 is promising for research of acute and chronic infections caused by planktonic bacteria .
Pol (476-484), HIV-1 RT Epitope is a biological active peptide. (This is a reverse transcriptase (RT) epitope (Pol residues 476-484). Within HIV-1 RT the peptide appears to be the dominant HLA A*0201-restricted epitope. Was used to investigate possible mechanisms behind HIV-1 escape from CTL. IV9 is the actual epitope processed and presented in HIV-1-infected cell lines.)
MCE RT Master Mix for qPCR II is a convenient, ready-to-use formulation for reverse transcription. With advanced reverse transcriptase, this kit can synthesize cDNA more rapidly, more specifically. The 100 rxns is defined as the base specification. All larger sizes correspond to incremental volumes of this base.
MCE RT Master Mix for qPCR II is a convenient, ready-to-use formulation for reverse transcription and can eliminate genomic DNA (gDNA) contaminations in RNA samples. With updated reverse transcriptase, this kit can synthesize cDNA more rapidly, more specifically. The 100 rxns is defined as the base specification. All larger sizes correspond to incremental volumes of this base.
MCE RT Master Mix for qPCR (gDNA digester plus) is a convenient, ready-to-use formulation for reverse transcription and can eliminate genomic DNA (gDNA) contaminations in RNA samples. The cDNA product can be directly applied as a template in a standard PCR and real time quantitative PCR (qPCR). The 100 rxns is defined as the base specification. All larger sizes correspond to incremental volumes of this base.
Anti-Mouse CD83 Antibody (Michel-17) is a rat-derived IgG1 κ type antibody inhibitor, targeting to mouse CD83. Anti-Mouse CD83 Antibody (Michel-17) can block CD83 and inhibit T cells proliferation. Anti-Mouse CD83 Antibody (Michel-17) can be used for the researches of cancer and immunology, such as solid tumor .
Anti-Mouse/Rat MHC Class II (I-Ek/RT1-D) Antibody (14-4-4S) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to mouse/rat MHC Class II. Anti-Mouse/Rat MHC Class II (I-Ek/RT1-D) Antibody (14-4-4S) reacts with mouse MHC Class II alloantigen I-Ek and the rat MHC class II alloantigen RT1D. Anti-Mouse/Rat MHC Class II (I-Ek/RT1-D) Antibody (14-4-4S) blocks antigen presentation. Anti-Mouse/Rat MHC Class II (I-Ek/RT1-D) Antibody (14-4-4S) can be used for the research of immunology and cancer .
Sennoside A is an anthraquinone glycoside found in senna (Cassia angustifolia). Sennoside A is an HIV-1 inhibitor (IC50=3.8 μM) that inhibits HIV-1 replication. Sennoside A also inhibits HIV-1 reverse transcriptase (RT)-related DNA polymerase (RDDP) and ribonuclease H (Ribonuclease H) with IC50s of 1.9 μM and 5.3 μM, respectively .
Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of EGFR, and thereby inhibits the downstream ERK and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR L858R/T790M mutation, and fungal infections .
Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs .
1,6-Di-O-galloyl-β-D-glucose is a compound found in the fruit of Phyllanthus emblica. 1,6-Di-O-galloyl-β-D-glucose has HIV-1 reverse transcriptase (RT) inhibitory activity with an IC50 value of 270 μM. The inhibitory mechanism of 1,6-Di-O-galloyl-β-D-glucose is competitive inhibition of the template primer and non-competitive inhibition of the substrate (dTTP). 1,6-Di-O-galloyl-β-D-glucose can be used in anti-HIV research .
Mer-NF5003E is a non-nucleoside reverse transcriptase inhibitor targeting HIV-1 reverse transcriptase (RT) (EC50=50 μM). Mer-NF5003E exhibits inhibitory activity against wild-type HIV-1 and multiple NNRTI-resistant strains (e.g., K103N, Y181C). Mer-NF5003E is promising for research of HIV infections .
Pseudoginsenoside RT5 (Standard) is the analytical standard of Pseudoginsenoside RT5. This product is intended for research and analytical applications. Pseudoginsenoside RT5 is isolated from Panax quinquefolium .
Luzopeptin A (BBM-928 A) is an actinoleukin-like antitumor antibiotic. Luzopeptin A is a bifunctional DNA intercalator which can interact with isolated DNA molecules. Luzopeptin A induces an unwinding-rewinding process of the closed superhelical PM2 DNA. Luzopeptin A is active against HIV-1 and HIV-2 reverse transcriptase with IC50s of 7 nM and 68 nM for HIV-1 RT and HIV-2 RT, respectively .
CI-39 is an antiviral natural product. CI-39 is an NNRTI (non-nucleoside reverse transcriptase inhibit) antiviral agent with an EC50 of 3.40 μM and an CC50 of >30 μM for wild type HIV-1. CI-39 inhibits HIV-1 RT DNA polymerase and ribonuclease H activitiessup .
Pseudoginsenoside RT4 is an orally active tetracyclic triterpenoid. Pseudoginsenoside RT4 can be isolated from Panax pseudoginseng subsp. Himalaicus. Pseudoginsenoside RT4 reduces the levels of pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β), boosts the levels of IL-10. Pseudoginsenoside RT4 modulates the composition of gut microbiota. Pseudoginsenoside RT4 shows anti-inflammatory effects. Pseudoginsenoside RT4 can be used in the study of ulcerative colitis .
Soulattrolide is a non-nucleoside HIV-1 reverse transcriptase (RT) inhibitor with IC50 values of 0.34 µM for HIV-1 RT, 69.5 µM for E. coliRNase H, and >495 µM for human DNA polymerase β, and can be found in Calophyllum teysmannii latex. Soulattrolide can be used for the research of HIV-1 infection, pain, inflammation, and Mycobacterium tuberculosis infection .
IL-1R2 is a competitive endogenous inhibitor of IL-1 signaling. IL-1R2 serves as a decoy receptor and competes with IL-1R1 for IL-1, it can also form a complex with IL-1RAP once it binds IL-1. IL-1R2 is implicated in various IL-1-mediated inflammatory diseases. IL-1R2 Protein, Human (HEK293, Fc) is a recombinant human IL-1R2 protein with an hFc tag at the C-terminus and is expressed in HEK293 cells. It consists of 330 amino acids (F14-E343).
The Gag-Pol polyprotein plays a central role in virion assembly, cooperating with Gag to bind to the plasma membrane, promote protein-protein interactions, recruit viral Env proteins, and package genomic RNA through direct interaction with the RNA packaging sequence (Psi). Gag-Pol polyprotein, HIV (440a.a, His) is the recombinant Virus-derived Gag-Pol polyprotein, expressed by E. coli , with N-6*His labeled tag.
The Gag-Pol polyprotein plays a central role in virion assembly, cooperating with Gag to bind to the plasma membrane, promote protein-protein interactions, recruit viral Env proteins, and package genomic RNA through direct interaction with the RNA packaging sequence (Psi). Gag-Pol polyprotein, HIV (560a.a, His) is the recombinant Virus-derived Gag-Pol polyprotein, expressed by E. coli , with N-6*His labeled tag.
IL-1R1 (CD121a) belongs to IL-1 receptor, and binds to IL-1α, IL-1β, IL-1Ra and IL-38 with comparable affinities (Kd: 0.1-1 nM). IL-1R1 regulates the transcription of multiple proinflammatory cytokines and mediates immune and inflammatory responses, including the activation of NF-κB and MAPK pathway. I IL-1R1 Protein, Human (HEK293) is a recombinant human extracellular region of IL-1R1 (M1-T332) without any tag, which is produced in HEK293 cells.
IL-1R1 (CD121a) belongs to IL-1 receptor, and binds to IL-1α, IL-1β, IL-1Ra and IL-38 with comparable affinities (Kd: 0.1-1 nM). IL-1R1 regulates the transcription of multiple proinflammatory cytokines and mediates immune and inflammatory responses, including the activation of NF-κB, MAPK pathways . IL-1R1 Protein, Rat (HEK293, His) is a recombinant rat extracellular region of IL-1R1 (M1-K352) with a C terminal His tag, which is produced in HEK293 cells.
IL-1R1 (CD121a) belongs to IL-1 receptor, and binds to IL-1α, IL-1β, IL-1Ra and IL-38 with comparable affinities (Kd: 0.1-1 nM). IL-1R1 regulates the transcription of multiple proinflammatory cytokines and mediates immune and inflammatory responses, including the activation of NF-κB and MAPK pathway. IL-1R1 Protein, Cynomolgus (HEK293, Fc) is a recombinant cynomolgus extracellular region of IL-1R1 (M1-T332) with a C-Terminal hFc tag, which is produced in HEK293 cells.
IL-1R1 (CD121a) belongs to IL-1 receptor, and binds to IL-1α, IL-1β, IL-1Ra and IL-38 with comparable affinities (Kd: 0.1-1 nM). IL-1R1 regulates the transcription of multiple proinflammatory cytokines and mediates immune and inflammatory responses, including the activation of NF-κB and MAPK pathway. IL-1R1 Protein, Cynomolgus (HEK293, His) is a recombinant cynomolgus extracellular region of IL-1R1 (M1-T332) with a C-Terminal His tag, which is produced in HEK293 cells.
IL-1R1 (CD121a) belongs to IL-1 receptor, and binds to IL-1α, IL-1β, IL-1Ra and IL-38 with comparable affinities (Kd: 0.1-1 nM). IL-1R1 regulates the transcription of multiple proinflammatory cytokines and mediates immune and inflammatory responses, including the activation of NF-κB and MAPK pathway. IL-1R1 Protein, Human (HEK293, Fc) is a recombinant human extracellular region of IL-1R1 (M1-T332) with a C-Terminal hFc tag, which is produced in HEK293 cells.
IL-1R1 (CD121a) belongs to IL-1 receptor, and binds to IL-1α, IL-1β, IL-1Ra and IL-38 with comparable affinities (Kd: 0.1-1 nM). IL-1R1 regulates the transcription of multiple proinflammatory cytokines and mediates immune and inflammatory responses, including the activation of NF-κB, MAPK pathways. IL-1R1 Protein, Rat (HEK293, His-mFc) is a recombinant rat extracellular region of IL-1R1 (M1-K352) with C terminal His and hFc tags, which is produced in HEK293 cells.
IL-1R1 (CD121a) belongs to IL-1 receptor, and binds to IL-1α, IL-1β, IL-1Ra and IL-38 with comparable affinities (Kd: 0.1-1 nM). IL-1R1 regulates the transcription of multiple proinflammatory cytokines and mediates immune and inflammatory responses, including the activation of NF-κB and MAPK pathway. IL-1R1 Protein, Human (HEK293, His) is a recombinant human extracellular region of IL-1R1 (L18-T332) with a C-Terminal 6*His tag, which is produced in HEK293 cells.
IL-1R1 (CD121a) belongs to IL-1 receptor, and binds to IL-1α, IL-1β, IL-1Ra and IL-38 with comparable affinities (Kd: 0.1-1 nM). IL-1R1 regulates the transcription of multiple proinflammatory cytokines and mediates immune and inflammatory responses, including the activation of NF-κB and MAPK pathway. IL-1R1 Protein, Mouse (HEK293, His) is a recombinant mouse extracellular region of IL-1R1 (L20-K338) with a C terminal 6*His tag, which is produced in HEK293 cells.
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively .
AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively .
Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Icotinib (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EFdA-TP is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP inhibits HIV-1RT with multiple mechanisms .
EFdA-TP tetrasodium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetrasodium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetrasodium inhibits HIV-1RT with multiple mechanisms . EFdA-TP (tetrasodium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EFdA-TP tetraammonium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetraammonium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetraammonium inhibits HIV-1RT with multiple mechanisms . EFdA-TP (tetraammonium) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Fozivudine tidoxil (BM-211290) is an orally active thioether lipid-zidovudine (ZDV) conjugate with anti-HIV activity. Fozivudine tidoxil, a member of the NRTI family of agent, is incorporated into the newly synthesized strand of DNA during intracellular viral replication and irreversibly binds viral RT which disrupts viral reverse-transcription . Fozivudine tidoxil is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity . 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
EGFR-IN-77 (Compound 4a) is a selective EGFR T790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFRT790M/L858R, 0.477 μM against EGFRL858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFRT790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFRL858R/T790M double-mutant non-small cell lung cancer .
Deoxyguanosine triphosphate (dGTP) trisodium solution (100 mM) is a nucleotide precursor in cells for DNA synthesis. Deoxyguanosine triphosphate trisodium salt is used in reverse transcription-polymerase chain reaction (RT-PCR) for DNA amplification .
Elvucitabine is an L-nucleoside analogue. Elvucitabine is a potent nucleoside reverse transcriptase (RT) inhibitor. Elvucitabine can be used in research of viral infection .
POMT1 Human Pre-designed siRNA Set A contains three designed siRNAs for POMT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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