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mutant selective

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Akt (9) Aminoacyl-tRNA Synthetase (1) Anaplastic lymphoma kinase (ALK) (1) Androgen Receptor (5) APC (2) Apoptosis (16) Atg8/LC3 (2) ATTECs (2) Autophagy (9) Bcr-Abl (1) BCRP (1) Biochemical Assay Reagents (1) BMX Kinase (1) Btk (3) c-Kit (5) c-Met/HGFR (1) Deubiquitinase (1) Drug Isomer (1) EGFR (56) Endogenous Metabolite (1) Epigenetic Reader Domain (2) ERK (4) Estrogen Receptor/ERR (3) Eukaryotic Initiation Factor (eIF) (1) Farnesyl Transferase (1) Ferroptosis (1) FGFR (4) FLT3 (6) GLUT (1) Glutathione Peroxidase (1) Glycosidase (1) GSK-3 (1) Histone Acetyltransferase (1) Histone Methyltransferase (5) HIV (7) HIV Protease (5) HSP (1) IRAK (3) Isocitrate Dehydrogenase (IDH) (20) Isotope-Labeled Compounds (5) JAK (1) Keap1-Nrf2 (1) LRRK2 (2) MAGL (1) MDM-2/p53 (2) MEK (3) Melanocortin Receptor (1) Mitophagy (1) mTOR (1) Organoid (3) PAK (1) Parasite (2) PARP (1) PD-1/PD-L1 (1) PDGFR (7) Phosphatase (2) Phosphodiesterase (PDE) (1) PI3K (6) Polo-like Kinase (PLK) (2) Potassium Channel (3) PROTACs (11) Proteasome (1) PTHR (1) Raf (7) Ras (25) Reactive Oxygen Species (2) RET (5) Reverse Transcriptase (1) ROS Kinase (3) SARS-CoV (5) SHP2 (1) Sodium Channel (1) STAT (2) TAM Receptor (1) Trk Receptor (1) VEGFR (2) γ-secretase (1)
By Research Areas:	Cancer (186) Cardiovascular Disease (2) Infection (8) Inflammation/Immunology (4) Metabolic Disease (4) Neurological Disease (10)
Click Chemistry:	Azide (2) Alkynes (4)

210

Inhibitors & Agonists

Peptides

Natural
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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19706

ARS-853 4 Publications Verification	Ras Apoptosis	Cancer
ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC₅₀ of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .

HY-10624

THIQ 1 Publications Verification	Melanocortin Receptor	Metabolic Disease
THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC₅₀=1.2 nM, EC₅₀=2.1 nM) and rMC4R (IC₅₀=0.6 nM, EC₅₀=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .

HY-157229

STX-721	EGFR	Others
STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants .

HY-19803

Naquotinib mesylate 5 Publications Verification ASP8273 mesylate	EGFR	Cancer
Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-19729

Naquotinib 5 Publications Verification ASP8273	EGFR	Cancer
Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-19985

PF-06459988	EGFR	Cancer
PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer .

HY-12872

Nazartinib 5+ Cited Publications EGF816	EGFR	Cancer
Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with K_i and K_inact of 31 nM and 0.222 min ⁻¹ on EGFR(L858R/790M) mutant, respectively.

HY-P3277

KRpep-2d	Ras	Cancer
KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .

HY-100476

Mutant IDH1-IN-3	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-3 (Compound 1) is a selective allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). Mutant IDH1-IN-3 has an IC₅₀ of 13 nM for R132H IDH1. Mutant IDH1-IN-3 inhibits the production of D-2-hydroxyglutaric acid (2HG) in cells. Mutant IDH1-IN-3 can be used in the study of cancer .

HY-100520

EGFR-IN-2	EGFR	Cancer
EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

HY-P3277A

KRpep-2d TFA	Ras	Cancer
KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .

HY-12872A

Nazartinib mesylate EGF816 mesylate	EGFR	Cancer
Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with K_i and K_inact of 31 nM and 0.222 min ^?1 on EGFR(L858R/790M) mutant, respectively.

HY-18690A

Enasidenib mesylate 10+ Cited Publications AG-221 mesylate	Isocitrate Dehydrogenase (IDH)	Cancer
Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.

HY-13984

Mutant EGFR inhibitor	EGFR	Cancer
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR ^L858R, EGFR ^{Exon 19 deletion} and EGFR ^T790M.

HY-13897

CNX-2006	EGFR	Cancer
CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC₅₀ below 20 nM for EGFR ^T790M.

HY-12408

6H05	Ras	Cancer
6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).

HY-160287

NVS MLLT-1	Epigenetic Reader Domain	Cancer
NVS MLLT-1 (compound 3) is a potent and selective MLLT1 inhibitor with K_d values of 0.18 µM, 0.24 µM, and 0.22 µM for wild-type, T1 mutants, and T3 mutants, respectively .

HY-W423595

BEBT-109	EGFR	Cancer
BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .

HY-131312

Crelosidenib LY3410738; mutant IDH1-IN-6	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC₅₀s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and *IDH2 R172K mutant* enzymes*, respectively. Mutant* IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .

HY-119177

PD173956	Bcr-Abl	Others
PD173956 is a pyridopyrimidine Bcr-Abl kinase inhibitor with high selectivity for the P-loop mutant form of Bcr-Abl .

HY-12408A

6H05 TFA	Ras	Cancer
6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).

HY-149359

IHMT-IDH1-053	Isocitrate Dehydrogenase (IDH)	Cancer
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible *IDH1-mutant* inhibitor with an IC₅₀ of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC₅₀=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .

HY-156681A

(S)-STX-478	PI3K	Cancer
(S)-STX-478 is the S-enantiomer of STX-478. STX-478 is a selective inhibitor of PI3Kα mutants, preventing metabolic dysfunction and demonstrating antitumor activity in xenograft mouse models with PI3Kα mutant tumors .

HY-18997

PLX7904 3 Publications Verification PB04	Raf	Cancer
PLX7904 is a potent and selective BRAF inhibitor, with IC₅₀ of appr 5 nM against BRAF ^V600E in mutant RAS expressing cells.

HY-15003

ATH686	FLT3 Apoptosis	Cancer
ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects .

HY-153306

RLY-2608	PI3K	Cancer
RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .

HY-12475

Mutant IDH1-IN-1 2 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC₅₀s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.

HY-18082

AGI-5198 15+ Cited Publications IDH-C35	Isocitrate Dehydrogenase (IDH)	Cancer
AGI-5198 (IDH-C35) is a potent and selective mutant IDH1 ^R132H inhibitor with an IC₅₀ of 0.07 μM.

HY-104036

IDH-305 1 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC₅₀= 27 nM (IDH1 ^R132H), 28 nM (IDH1 ^R132C), 6.14 µM (IDH1 ^WT)) .

HY-154959

AZD4747	Ras	Cancer
AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS ^G12C inhibitor. AZD4747 has the potential to study cancer .

HY-111050

JNJ-38877618	c-Met/HGFR	Cancer
JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC₅₀s of 2 and 3 nM for wild type and mutant Met, respectively.

HY-125841

EGFR mutant-IN-1	EGFR	Cancer
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) .

HY-128860

Mutated EGFR-IN-2	EGFR	Cancer
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 .

HY-128589

CHMFL-KIT-033	c-Kit	Cancer
CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC₅₀ of 0.045 μM .

HY-154313

Spiclomazine Clospirazine	Ras	Cancer
Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .

HY-100002

ML162 5+ Cited Publications	Glutathione Peroxidase Ferroptosis	Cancer
ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines

HY-141807

MS21	PROTACs Akt	Cancer
MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.

HY-146223

AZD4625	Ras	Cancer
AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS ^G12C. AZD4625 has high oral bioavailability .

HY-117540

ZLD10A	Histone Methyltransferase	Cancer
ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .

HY-136379

CID44216842 1 Publications Verification Cdc42-IN-1	Ras	Cancer
CID44216842 (Cdc42-IN-1) is a potent *Cdc42*-selective guanine nucleotide binding lead inhibitor. The EC₅₀s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC₅₀s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe .

HY-19617A

EGFR-IN-1 hydrochloride	EGFR	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 .

HY-13810

PF-04880594	Raf	Cancer
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 .

HY-168876

AZ14240475	EGFR	Cancer
AZ14240475 is a potent, selective, and brain-penetrant inhibitor of EGFR Ex20Ins mutants, with the pIC₅₀ of 7.6. AZ14240475 plays an important role in cancer research .

HY-135805A

(Rac)-JBJ-04-125-02	EGFR	Cancer
(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor .

HY-13237

GSK2578215A 2 Publications Verification	LRRK2 Autophagy Mitophagy	Neurological Disease Cancer
GSK2578215A is a potent and highly selective LRRK2 inhibitor, which exhibits IC₅₀s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.

HY-19617B

EGFR-IN-1 TFA	EGFR	Cancer
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 .

HY-19617

EGFR-IN-1	EGFR	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 .

HY-112256

ACP-105 5 Publications Verification	Androgen Receptor	Inflammation/Immunology
ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC₅₀s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.

HY-164315

KRAS G12C inhibitor 67	Ras	Cancer
KRAS G12C inhibitor 67 (example 35) is a KRAS G12C inhibitor that selectively inhibits the growth of many KRAS G12C mutant tumor cell lines .

HY-130253

IRAK4-IN-6	IRAK	Cancer
IRAK4-IN-6 is an orally efficacious and selective IRAK4 inhibitor with an IC₅₀ of 4 nM, and targetes MyD88 L265P mutant diffuse large B cell lymphoma .

Cat. No.	Product Name	Target	Research Area

HY-P3277

KRpep-2d	Ras	Cancer
KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .

HY-P3277A

KRpep-2d TFA	Ras	Cancer
KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-130259

LC3-mHTT-IN-AN2	Structural Classification other families Source classification Coumarins Phenols Polyphenols Phenylpropanoids Plants	Atg8/LC3 ATTECs Autophagy
LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons .

HY-N12390

Alternaphenol B2	Structural Classification Microorganisms Source classification Phenols Polyphenols	Isocitrate Dehydrogenase (IDH)
Alternaphenol B2 is a selective IDH1 inhibitor from the coral-derived fungus Parengyodontium album SCSIO SX7W11. Alternaphenol B2 shows inhibitory activity against isocitrate dehydrogenase mutant R132H (IDH1m), with IC₅₀ values of 41.9 μM .

Cat. No.	Product Name	Chemical Structure

HY-15772S1

Osimertinib-13C,d3
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.

HY-15772S

Osimertinib-d6
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[1].

HY-14588S

(rel)-Lopinavir-d8

(rel)-Lopinavir-d₈ ((rel)-ABT-378-d₈) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 14.2 μM .

HY-114436S

MRTX-1257-d6
MRTX-1257-d₆ is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC₅₀ of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .

HY-18690S

Enasidenib-d6
Enasidenib-d₆ (AG-221-d₆) is the deuterium labeled Enasidenib (HY-18690) . Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC₅₀s of 100 and 400 nM against IDH2 ^R140Q and IDH2 ^R172K, respectively .

HY-151903S

FGFR2/3-IN-1
FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].

HY-14588S2

Lopinavir-d7

Lopinavir-d₇ is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 14.2 μM .

HY-14588S1

Lopinavir-d8
Lopinavir-d₈ (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].

Cat. No.	Product Name		Classification

HY-134813

MRTX1133 20+ Cited Publications		Alkynes
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .

HY-104066

Theliatinib Xiliertinib; HMPL-309		Alkynes
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a K_i of 0.05 nM and an IC₅₀ of 3 nM. Theliatinib has an IC₅₀ of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-159493

BI2536-PEG2-Halo		Azide
BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC₅₀=23 nM), exhibits selective toxicity against p53 mutant cancer cells .

HY-104066A

Theliatinib tartrate Xiliertinib tartrate; HMPL-309 tartrate		Alkynes
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a K_i of 0.05 nM and an IC₅₀ of 3 nM. Theliatinib has an IC₅₀ of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-172140

Ebio3		Alkynes
Ebio3 is a selective potassium channel (KCNQ2) inhibitor with an IC₅₀ of 1.2 nM. Ebio3 binds to the KCNQ2 channel through its hydrophobic tail, causing the S6 helix to move inward, which leads to the closure of the inner gate. The inhibitory effect of Ebio3 is also effective in pathogenic mutants of KCNQ2 (such as R75C and I238L), where it can inhibit outward currents by more than 80%. Ebio3 is expected to be used in the research of neurological diseases such as epilepsy .

HY-152233

Reverse transcriptase-IN-4		Azide
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC₅₀ value of 0.053 μM for wild-type HIV-1 and an EC₅₀ value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 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.

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