Ras Control

Sotorasib (AMG-510) isomer is the less active isomer of Sotorasib (AMG-510). AMG-510 is a potent KRAS G12C covalent inhibitor.

(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

(9R,12aR)-AZD4747 is a diastereomer of AZD4747 (HY-154959). AZD4747 is a selective mutant GTPase KRAS^G12C inhibitor with blood-brain barrier permeability. AZD4747 has the potential to study cancer.

(S)-BAY-293 is a negative control of BAY 293. BAY 293 is a potent KRAS-SOS1 interaction inhibitor.

Scrambled Tadnersen is the Negative Control of Tadnersen sodium (HY-132581A). Tadnersen sodium, an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion.

(Rac)-D3S-001 is the racemate of D3S-001 (HY-160023).

TAT-PAK18 R192A is an inactive Tat-Pak peptide. TAT-PAK18 R192A does not have any effect in the translocation of Rac1 triggered by any of the interrogated proteins.

Scrambled Tadnersen sodium is the Negative Control of Tadnersen sodium (HY-132581A). Tadnersen sodium, an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion.

(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRAS^G12C inhibitor with an IC₅₀ of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRAS^G12C mutations. AZD4625 can be used for the study of KRAS^G12C mutant non-small cell lung cancer.