From 11:00 pm to 12:00 pm EST ( 8:00 pm to 9:00 pm PST ) on January 6th, the website will be under maintenance. We are sorry for the inconvenience. Please arrange your schedule properly.
B-Raf IN 11 (ZINC72115182) is a selective B-RafV600E inhibitor (IC50=76 nM), shows selectivity for B-RafV600E over B-RafWT with selectivity of 3.1-fold. B-Raf IN 11 can be used in colorectal cancer research [1]
B-Raf IN 15 (Compound 7) is a BRAF inhibitor. B-Raf IN 15 inhibits BRAF WT and BRAF V600E with IC50s of 2.0 and 0.8 μM. B-Raf IN 15 can be used for the research of cancer [1].
B-Raf IN 5 (compound 3b) is a potent inhibitor of protein kinase B-Raf with an IC50 of 2.0 nM. B-Raf IN 5 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease [1].
B-Raf IN 6 (compound 2c) is a potent inhibitor of protein kinase B-Raf with an IC50 of 1.7 nM. B-Raf IN 6 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease [1].
B-Raf IN 13 is a BRAF inhibitor with an IC50 of 3.55 nM in BRAF V600E enzyme assay. B-Raf IN 13 has anticaner effects (WO2020261156A1, Example 74) [1].
B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM [1].
B-Raf IN 2 is a potent and selective BRAF inhibitor extracted from patent WO2021116055A1, compound Ia. B-Raf IN 2 can be used for the research of cancer [1].
PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity [1].
B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer [1].
B-Raf IN 8 (compound 7g) is a potent B-Raf inhibitor, with an IC50 of 70.65 nM. B-Raf IN 8 exhibits antitumor activity against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells, with IC50 values of 9.78, 13.78, 18.52 and 29.85 µM [1].
B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor, with an IC50 of 110.23 nM. B-Raf IN 7 exhibits antitumor activity against colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela) and human prostate cancer (PC-3) cells, with IC50 values of 7.50, 9.87, 10.57, 11.63 and 12.83 µM [1].
B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
IDE2 is a small molecule cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) by activating the TGF-βsignaling pathway[1].
IDE Human Pre-designed siRNA Set A contains three designed siRNAs for IDE gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively [1].
Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity [1].
EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent EGFR/BRAF inhibitor with an IC50 of 45 nM for BRAFV600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI50=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity [1].
PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.
RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAFV600E and B-RAFWT, respectively [1].
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAFV600E and BRAFWT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase [1].
HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells.
SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAFV600E and BRAFWT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase [1].
PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth [1].
PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth [1].
MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR WTIC50=281 nM, c-MET IC50=205 nM, B-RAFWTIC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR T790MIC50=69 nM and B-RAFV600EIC50=83 nM) [1].
BRAF Human Pre-designed siRNA Set A contains three designed siRNAs for BRAF gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Braf Mouse Pre-designed siRNA Set A contains three designed siRNAs for Braf gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Braf Rat Pre-designed siRNA Set A contains three designed siRNAs for Braf gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
BRAFV600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAFV600E/CRAF. BRAFV600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAFV600E/CRAF-IN-1 has the potential for the research of cancer diseases [1].
BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAFV600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases [1].
LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 [1].
Sorafenib-d4 is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities [1].
Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv 600E and C-RAF respectively [1].
Raf inhibitor 3 (Example 30) is a Raf inhibitor. Raf inhibitor 3 inhibits B-Raf and C-Raf with IC50 values less than 15 nM. Raf inhibitor 3 can be used for research of cancers [1].
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively [1] . Vemurafenib induces cell autophagy .
6bK TFA is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK TFA increases circulating insulin in high-fat-fed mice. Acute administration of 6bK TFA enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice [1].
Sorafenib-d3 (Donafenib), a deuterated compound of Sorafenib, is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively [1].
AWL-II-38.3 is a potent ephrin-A receptor (EphA3) kinase inhibitor. AWL-II-38.3 does not exhibit significant cellular activity against Src-family kinases nor against b-raf[1][1] .
Vemurafenib-d5 is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy[1] .
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 µM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue [1].
Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator [1].
Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator [1].
Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM [1] .
ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers [1].
PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of B-RafV600E with an IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf[1][2].
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research [1] .
OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K + channels and has Ca 2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation [1].
OR-1855, an active metabolite of Levosimendan, has effect on human myometrial contractility. Levosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure [1] .
Nitecapone (OR-462) is an orally active and short-acting catechol-O-methyltransferase (COMT) inhibitor with gastroprotective and antioxidant properties. Nitecapone (OR-462) scavenges reactive oxygen and nitric radicals and prevents lipid peroxidation [1] .
ML345 is a potent and selective insulin-degrading enzyme (IDE) small-molecule inhibitor, with an IC50 value of 188 nM. ML345 can be for use as a pharmacophore for agent development in diabetes research [1].
Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC ™) degrader of BRAFV600E with a DC50 of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAFV600E splice variant. CFT1946 can be used in tumor research [1] .
Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively [1] .
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity [1].
Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC50s of 4.25 and 2.7 nM for BRAFV600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies [1].
AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity [1].
RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAFwt, and bRAFV600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAFV600E mutation, respectively [1].
BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases [1].
NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors [1].
3,5-Dinitrocatechol (OR-486) is a potent catechol-O-methyltransferase inhibitor, with an IC50 of 12 nM. 3,5-Dinitrocatechol can be used in the preparation of the molybdenum (VI)- 3,5-Dinitrocatechol complex [1] .
OR1A1 Human Pre-designed siRNA Set A contains three designed siRNAs for OR1A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR1A2 Human Pre-designed siRNA Set A contains three designed siRNAs for OR1A2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR2AT4 Human Pre-designed siRNA Set A contains three designed siRNAs for OR2AT4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR2H1 Human Pre-designed siRNA Set A contains three designed siRNAs for OR2H1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR2M7 Human Pre-designed siRNA Set A contains three designed siRNAs for OR2M7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR4F17 Human Pre-designed siRNA Set A contains three designed siRNAs for OR4F17 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR4F5 Human Pre-designed siRNA Set A contains three designed siRNAs for OR4F5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR51E1 Human Pre-designed siRNA Set A contains three designed siRNAs for OR51E1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR51E2 Human Pre-designed siRNA Set A contains three designed siRNAs for OR51E2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR5B21 Human Pre-designed siRNA Set A contains three designed siRNAs for OR5B21 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR6A2 Human Pre-designed siRNA Set A contains three designed siRNAs for OR6A2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
OR7D4 Human Pre-designed siRNA Set A contains three designed siRNAs for OR7D4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
DOG-IM4 can be used to synthesize nanoparticles to deliver antigen-encoding nucleic acids. It could be used to try to target autoimmune diseases, rare blood or metabolic diseases, allergies, cancer or infectious diseases [1].
Vem-L-Cy5 (compound 3)，modified with the NIR fluorophore cyanine-5 (Cy5)，is a Vemurafenib (HY-12057)-based inhibitor of BRAF. Vem-L-Cy5 targets to BRAFV600E，and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability，and inhibits cell growth of many types of cancer [1].
Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively [1].
RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively [1]. Antitumor efficacy [1].
Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
Lifirafenib (BGB-283) maleate is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively [1].
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAFwt, and bRAFV600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively [1].
PF-04880594 is a potent and selective RAF inhibitor. PF-04880594 inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 shows antitumor activity [1].
SJF-0628 (compound 512) is a PROTACRAF degrader. SJF-0628 induces targeted degradation of BRAF mutants (DC50: 5.4 nM, 4.64 nM, 15.5 nM, 2.11 nM, 63.9 nM for BRAF V600E, V600K, G464V, G469A, K601E respectively). SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of disorders that result from aggregation or accumulation of RAF, or the constitutive activation of RAF [1].
Anticancer agent 124 is an orally active, highly selective and potent pan RAF inhibitor. Anticancer agent 124 inhibits MAPK signalling in BRAF V600E, NRAS and KRAS mutant tumor cells [1].
ARN22089 is a oral active novel class of trisubstituted pyrimidine, blocks the interaction of CDC42 GTPases with specific downstream effectors. ARN22089 blocks tumor growth in BRAF mutant mouse melanoma model [1].
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations [1].
Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity [1] .
PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research [1].
Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF[1] .
Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF[1] .
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma [1].
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers [1].
IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent IRE-1α inhibitor. IRE1α kinase-IN-8 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) [1].
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research [1] .
Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively [1].
MSN-50 is a Bax and Bak oligomerization inhibitor. MSN-50 efficiently inhibits liposome permeabilization, prevents genotoxic cell death and promotes neuroprotection [1] .
EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma [1].
L-156602 is a C5a receptor antagonist. L-156602 inhibits inflammation, and the migration of monocytes and neutrophils to the infiltrating site in mouse inflammatory models. L-156602 suppresses the efferent phase of delayed-type hypersensitivity (DTH) [1] .
Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity [1].
Rafoxanide (Standard) is the analytical standard of Rafoxanide. This product is intended for research and analytical applications. Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research [1] .
Mosunetuzumab (BTCT-4465A) is a full-length, fully humanized immunoglobulin G1 (IgG1) T-cell-dependent bispecific (TDB) antibody targeting CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used for the research of relapsed or refractory (R/R) B-cell non-Hodgkin lymphomas (B-NHLs) [1] .
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia [1] .
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAFV600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively [1].
Monalizumab (IPH2201) is an immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC) [1] .
BC15 aptamer sodium is an ssDNA aptamer targeting the intracellular protein hnRNP A1, which is highly expressed in cancerous liver tissue. BC15 aptamer sodium specifically recognizes breast cancer cells and can be used to detect cancer cells in other pathological types of breast cancer tissue [1].
Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers.
As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy.
MCE offers a unique collection of 1835 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF[1] .
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia [1] .
Mosunetuzumab (BTCT-4465A) is a full-length, fully humanized immunoglobulin G1 (IgG1) T-cell-dependent bispecific (TDB) antibody targeting CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used for the research of relapsed or refractory (R/R) B-cell non-Hodgkin lymphomas (B-NHLs) [1] .
Monalizumab (IPH2201) is an immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC) [1] .
Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively [1].
Insulin/IDE protein is the key to the decomposition of cellular peptides. It participates in the degradation of insulin, APP peptides, IAPP peptides, natriuretic peptides, glucagon, bradykinin, kinins and other peptides, and affects intercellular peptide signaling. Substrate binding induces conformational changes that promote degradation of larger substrates such as insulin. Insulysin/IDE Protein, Human (HEK293, His) is the recombinant human-derived Insulysin/IDE protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Insulysin/IDE Protein, Human (HEK293, His) is 978 a.a., with molecular weight of ~120.0 kDa.
OR13A1 operates as an odorant receptor. OR13A1 Protein, Human (Cell-Free, His) is the recombinant human-derived OR13A1 protein, expressed by E. coli Cell-free, with N-10*His labeled tag. The total length of OR13A1 Protein, Human (Cell-Free, His) is 328 a.a., with molecular weight of 39.3 kDa.
OR5AL1 operates as an odorant receptor. OR5AL1 Protein, Human (Cell-Free, His) is the recombinant human-derived OR5AL1 protein, expressed by E. coli Cell-free, with N-10*His labeled tag. The total length of OR5AL1 Protein, Human (Cell-Free, His) is 328 a.a., with molecular weight of 39.6 kDa.
OR5V1 serves as an odorant receptor. OR5V1 Protein, Human (Cell-Free, His) is the recombinant human-derived OR5V1 protein, expressed by E. coli Cell-free, with N-10*His labeled tag. The total length of OR5V1 Protein, Human (Cell-Free, His) is 321 a.a., with molecular weight of 42.1 kDa.
The OPRD1 protein is a G protein-coupled receptor for enkephalins and opioids that undergoes ligand-induced conformational changes to activate signaling through G proteins and inhibit adenylate cyclase. Additionally, it reduces neurotransmitter release by affecting ionic currents. OPRD1 Protein, Human (Cell-Free, His) is the recombinant human-derived OPRD1 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of OPRD1 Protein, Human (Cell-Free, His) is 372 a.a., with molecular weight of 41.9 kDa.
The Serpin B6b Protein, an integral serpin family member, plays a crucial role as a serine protease inhibitor, regulating proteolytic activities. Its study enhances understanding of cellular processes related to proteolysis, with therapeutic applications. The classification within the serpin family emphasizes unique mechanisms and substrate specificity, providing insights into broader impacts on cellular processes. Further exploration of Serpin B6b's role promises to enhance knowledge of its contributions to both normal physiology and pathological conditions. Serpin B6b Protein, Mouse (sf9, His) is the recombinant mouse-derived Serpin B6b protein, expressed by Sf9 insect cells, with C-His labeled tag. The total length of Serpin B6b Protein, Mouse (sf9, His) is 377 a.a., with molecular weight of ~43 kDa.
The OGG1 protein is a DNA repair enzyme specifically designed to cleave DNA at the 8-oxoG residue and plays a key role in maintaining genome integrity. It demonstrates the ability to excise damaged bases such as 7,8-dihydro-8-oxoguanine and 2,6-diamino-4-hydroxy-5-N-methylformamidopyrimidine from the DNA structure (FAPY). OGG1 Protein, Human (GST) is the recombinant human-derived OGG1 protein, expressed by E. coli , with tag free. The total length of OGG1 Protein, Human (GST) is 345 a.a., with molecular weight of ~38.0 kDa.
KMT2D Protein, a histone methyltransferase, methylates histone H3 'Lys-4' (H3K4), predominantly establishing H3K4me1 marks at active chromatin sites. Integral to chromatin remodeling, it functions as a coactivator for the estrogen receptor, recruited by ESR1, activating transcription. KMT2D's role in depositing specific histone marks at genomic locations underscores its crucial involvement in modulating chromatin structure and gene expression. KMT2D Protein, Human is the recombinant human-derived KMT2D protein, expressed by E. coli , with tag free. The total length of KMT2D Protein, Human is 155 a.a., .
KMT2D Protein, a histone methyltransferase, methylates histone H3 'Lys-4' (H3K4), predominantly establishing H3K4me1 marks at active chromatin sites. Integral to chromatin remodeling, it functions as a coactivator for the estrogen receptor, recruited by ESR1, activating transcription. KMT2D's role in depositing specific histone marks at genomic locations underscores its crucial involvement in modulating chromatin structure and gene expression. KMT2D Protein, Human (GST) is the recombinant human-derived KMT2D protein, expressed by E. coli , with N-GST labeled tag. The total length of KMT2D Protein, Human (GST) is 155 a.a., .
IMPA1 protein provides essential inositol for the synthesis of phosphatidylinositol and polyphosphate inositol. IMPA1 Protein, Human (His) is the recombinant human-derived IMPA1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of IMPA1 Protein, Human (His) is 277 a.a., with molecular weight of ~30.0 kDa.
IMPA2, or Inositol monophosphatase 2, demonstrates enzymatic activity by utilizing various substrates such as myo-inositol monophosphates, scylloinositol 1,4-diphosphate, glucose-1-phosphate, beta-glycerophosphate, and 2'-AMP. Additionally, it has been implicated as the pharmacological target for the action of lithium ions (Li⁺) in the brain. IMPA2 Protein, Human (His) is the recombinant human-derived IMPA2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of IMPA2 Protein, Human (His) is 288 a.a., with molecular weight of ~30.0 kDa.
The Serpin B3 protein exhibits versatility in cellular regulation and may act as a papain-like cysteine protease inhibitor to modulate immune responses against tumor cells. Its dual role extends to inhibiting UV-induced apoptosis by inhibiting c-Jun NH(2)-terminal kinase (JNK1) activity, suggesting that Serpin B3 is involved in the stress response. Serpin B3 Protein, Human (HEK293, His) is the recombinant human-derived Serpin B3 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Serpin B3 Protein, Human (HEK293, His) is 390 a.a., with molecular weight of 41-50 kDa.
Sorafenib-d3 (Donafenib), a deuterated compound of Sorafenib, is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively [1].
Sorafenib-d4 is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
Vemurafenib-d5 is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of B-RafV600E with an IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf[1][2].
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
B-Raf Antibody is a non-conjugated and Mouse origined monoclonal antibody about 84 kDa, targeting to B-Raf. It can be used for WB,IHC-P,ICC assays with tag free, in the background of Human, Mouse, Rat.
BRAF Antibody is a non-conjugated and Mouse origined monoclonal antibody about 84 kDa, targeting to BRAF (4E1). It can be used for WB assays with tag free, in the background of Human, Mouse.
Phospho-BRAF (Thr401) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 84 kDa, targeting to Phospho-BRAF (Thr401). It can be used for WB,IP assays with tag free, in the background of Human, Mouse, Rat.
KDM1A; AOF2; KDM1; KIAA0601; LSD1; Lysine-specific histone demethylase 1A; Braf35-HDAC complex protein BHC110; Flavin-containing amine oxidase domain-containing protein 2
WB
Human, Mouse, Monkey
KDM1A Antibody (YA718) is a non-conjugated and Mouse origined monoclonal antibody about 93 kDa, targeting to KDM1A (1B2). It can be used for WB assays with tag free, in the background of Human, Mouse, Monkey.
